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FEW PUBLICATIONS WITH GA FULL LIST OF PUBLICATIONS [LINK]
Recent | 2006-2008 | 2000-2005
Recent: 2009 - Present ● A Systematic Review of the Efficacy and Safety of Favipiravir (Avigan) for the Treatment of Novel COVID-19 Infections ●Bag*, Subhendu Sekhar; Sinha, Sayantan; and Saito, Isao ● Medical Research Archives 2020, XX, XX (In Press).
● Wastewater an Emerging Source of Spreading COVID-19 Infections in India: A Recent Perspective● Bag*, Subhendu Sekhar and Sinha, Sayantan● Current Science 2020, XX, XX (Under Review).
● Inhibiting the Pathogenicity of SARS-CoV-2 with a Designer Fluorescent Carbon Quantum Dot (FL-ASCQD): A Concept● Bag*, Subhendu Sekhar and Sinha, Sayantan● Medicinal Chemistry 2020, XX, XX (Under Review).
● SARS-CoV-2 from Host Cell Entry, Pathogenicity to Possible Remediation of the Infection Caused: An Overview● Bag*, Subhendu Sekhar and Sinha, Sayantan● 2020, XX, XX (Communicated).
● Stabilization of an Abasic Site Paired Against an Unnatural Triazolyl Nitrobenzene Nucleoside● Bag*, Subhendu Sekhar; Sinha, Sayantan; Gogoi, Hiranya; Datta, Subhashis; Kundu, Rajen; Talukdar, Sangita● Biophysical Chemistry 2020, XX, XX (In Press).
● Extended fluorescent uridine analogues: Synthesis, photo-physical properties and selective interaction with BSA protein● Ardhapure, Ajaykumar V.; Gayakhe, Vijay; Bhilare, Shatrughn; Kapdi*; Anant R.; Bag*, Subhendu Sekhar; Sanghvi,Yogesh S.; Gunturu, Krishna Chaitanya● New Journal of Chemistry 2020, XX, XX (Under Revision).
78. ● Triazolyl C-Nucleosides via the Intermediacy of β-1'-ethynyl-2'-deoxyriboside Derived from a Nicholas Reaction: Synthesis, Photophysical Property and Interaction with BSA†● Bag*, Subhendu Sekhar; Das, Suman, K.● J. Org. Chem. 2018, XX, XX (Under Revision).
77.● Pyrenylthioureayl Alanine as a Switch-on Fluorescent Sensor for Hg(II) Ions● Bag*, Subhendu Sekhar; De, Suranjan● Chemistry Select. 2018, 3, 11758-11764.
76.● Synergized AgNPs formation using microwave in a bio-mediated route: Studies on particle aggregation and electrocatalytic sensing of ascorbic acid from biological entities● Dash, S. R.; Bag, S. S.; Golder, K. A.● J. Electroanal. Chem. 2018, 827, 181–192.
75.●Relay FRET Event in a Designed Trichromophoric Pentapeptide Containing o-, m-Aromatic-Amino Acid Scaffold ● Bag*, Subhendu Sekhar; Yashmeen, Afsana● Chem. Commun. 2018, 54, 9765-9768.
74.●Virtual Screening, Molecular modelling and biochemical studies to exploit PF14_0660 as a target to identify novel anti-malarials●Vimee Raturi1, Kumar Abhishek1, Subhashis Jana2, Subhendu Sekhar Bag2 and Vishal Trivedi1 ●Letters in Drug Design & Discovery 2018, XX, XX (In Press).
73.●Green Synthesis of Silver Nanoparticle using Sechium Edule Fruit Aqueous Extract and Study of Antimicrobial and Catalytic Activity ● Bag*, Subhendu Sekhar; Banerjee, Ankita; Singh, Anu; Golder, Animes Kumar; Bora, Anupama ● Current Nanomaterials, 2018, (In Press).
72.●Book Chapter: ● Sonogashira Cross-Coupling: Alkyne-modified Nucleosides and their Applications, ch 4. ● Bag*, Subhendu Sekhar, Jana, Subhashis; Kasula Mohan● In Palladium-Catalyzed Modification of Nucleosides, Nucleotides and Oligonucleotides, Eds. Kapdi, A. R; Maiti, D.; Sanghvi, Y. S. Publisher: Elsevier, 2018 (ISBN: 9780128112922).
71.●Design of “Click” Fluorescent Labelled 2′-deoxyuridines via C5-{4-(2-Propynyl(methyl)amino)}phenyl acetylene as a Universal Linker: Synthesis, Photophysical Property and Interaction with BSA†● Bag,* Subhendu Sekhar and Hiranya Gogoi● JOC, 2018, 83, 7606-7621.
70.●Synthesis of furan-fused 1,4-dihydrocarbazoles via an unusual Garratt-Braverman Cyclization of indolyl propargyl ethers and their antifungal activity● Mandal, A.; Mandal, S. M.; Jana, S.; Bag,* Subhendu Sekhar; Basak, A. ●Tetrahedron, 2018, 74, 3543-3556.
69.●Design of a Fused Triazolyl 2-Quinolinone Unnatural Nucleoside via a Tandem CuAAC-Ullmann Coupling Reaction and Study of Photophysical Property● Bag,* Subhendu Sekhar; Das, Suman Kalyan; Gogoi, Hiranya● Tetrahedron 2018, 74, 2218.
68.●Multipurpose Isothiocyanyl Alanine/Lysine: Use as Solvatochromic IR Probes and in Site Specific Labeling/Ligation of Short Peptides● Bag,* Subhendu Sekhar; De, Suranjan● Bioorganic and Medicinal Chemistry Letters 2018, 28, 1404.
67.●Sensing the Chemical Cleavage of Fluorescent β-Lactams via FRET/Exciplex or Excimer Emission● Bag,* Subhendu Sekhar; Afsana Yashmeen● J. Phochem.Photobiol. A:Chemistry 2017, 353, 464-468.
66.●Uracil-Amino Acid as a Scaffold for β-Sheet Peptidomimetics: Study of Photophysics and interaction with BSA Protein ● Bag,* Subhendu Sekhar; Afsana Yashmeen● Bioorganic and Medicinal Chemistry Letters 2017, 27, 5387.
65.●Use of Azido Naphthalimide Carboxylic Acids as Fluorescent Template with Built-in Photo-reactive Group and Flexible Linker Simplifies Protein Labeling Study: Applications in Selective Tagging of HCAII and Penicillin Binding Proteins ● Bag, Subhendu Sekhar;● Chemical Communications 2017, 53, 13015 (Outside Back Cover Page; DOI: 10.1039/C7CC08209F).
64.●Tetrazolylpyrene Unnatural Nucleoside as a Human Telomeric Multimeric G-Quadruplex Selective Switch-On Fluorescent Sensor ● Bag,* Subhendu Sekhar; Manoj Kumar Pradhan, Talukdar, Sangita● Organic and Biomolecular Chemistry 2017, 15, 10145.
63.●Isothiocyanyl Alanine as a Synthetic Intermediate for the Synthesis of Thioureayl Alanines and Subsequent Aminotetrazolyl Alanines ● Bag,* Subhendu Sekhar; Suranjan De● The Journal of Organic Chemistry 2017, 82, 12276.
62.●Axially Chiral Amino Acid Scaffold as an Efficient Fluorescent Discriminator of Methanol-Ethanol● Bag,* Subhendu Sekhar; Jana, Subhashis● New Journal of Chemistry 2017, 41, 13391-13398.
61.●Trifunctional fluorescent unnatural nucleoside: Label free detection of T-T/C-C base mismatches, abasic site and bulge DNA● Bag,* Subhendu Sekhar; Manoj Kumar Pradhan, Talukdar, Sangita● J. Photochem. Photobiol. B 2017, 173, 165-169.
60.●Design, Synthesis and Photophysical Property of a Doubly Widened Fused-Triazolyl-Phenanthrene Unnatural Nucleoside● Bag,* Subhendu Sekhar; Das, Suman Kalyan● Chemistry Select 2017, 2, 3577-3583.
59.●A Bio-synthesis Route to nearly spherical AgNPs using Chayote fruit extract ● Rao, Ch. Venkatanarasimha; Bag, Subhendu Sekhar; Golder, Animes Kumar ● Environmental Progress & Sustainable Energy 2017, 36, 192.
58.●Bis-Pyridobenzene as A Fluorescence Light-up Sensor for Hg2+Ion in Water● Ghosh, Ujjal, Bag,* Subhendu Sekhar; Mukherjee,* Chandan● Sensors & Actuators: B. Chemical 2017, 238, 903.
57.●Hybridization Accompanying FRET Event in Labeled Natural Nucleoside-Unnatural Nucleoside Containing Chimeric DNA Duplexes ● Bag*, Subhendu Sekhar; Das, Suman Kalyan; Pradhan, Monoj Kumar; Jana, Subhashis● Journal of Photochemistry & Photobiology, B: Biology 2016, 162, 669-673.
56. Book Chapter: ●Design of Environmentally Sensitive Fluorescent Nucleosides and Their Applications● Bag*, Subhendu Sekhar; Saito, Isao; ● In Fluorescent Analogues of Biomolecular Building Blocks: Design and Applications, Eds. Tor, Yitzhak; Wilhelmsson, Marcus. Publisher: John Wiley & Sons (2016). (ISBN: 978-1-118-17586-6).
55.●Mechanistic studies on Garratt-Braverman Cyclization: Solving the Diradical-Cycloaddition Puzzle ● Das, Joyee; Bag,* Subhendu Sekhar; Basak*, Amit● J. Org. Chem. 2016, 81(11), 4623.
54.●Synthesis and Photophysical Properties of Triazolyl-Donor/Acceptor Chomophores Decorated Unnatural Amino Acids and Application of Triazolylperylene Amino Acid in Sensing BSA● Bag,* Subhendu Sekhar; Jana, Subhashis; Pradhan, Manoj Kumar● Bioorg. Med. Chem. 2016, 24(16), 3579.
53.●Donor/Acceptor Chromophores Decorated Triazolyl Unnatural Nucleosides: Synthesis, Photophysical Properties and Study of Interaction with BSA● Bag,* Subhendu Sekhar; Talukdar, Sangita; Das, Suman Kalyan; Pradhan, Manoj Kumar; Mukherjee, Soumen ● Org. Biomol. Chem. 2016, 14, 5088.
52.●Trichromophoric
Pentapeptide:
Impact of
β-Sheet Conformation on Dual Path to Excimer Emission
and Sensing of BSA Protein
● Bag,*
Subhendu Sekhar; Jana, Subhashis; Pradhan, Manoj
Kumar;
Pal, Sunit●
RSC Advances
2016, 6, 72654.
Abstract: We are reporting a dual door entry system to excimer emission in a designed triazolo amino acid scaffolded (ArTAA) trichromophoric b-sheet pentapeptide. In our design, two fluorescent unnatural amino acids (TPyAlaDo) are embedded into two arms of a novel chromophoric scaffold, ArTAA, via an intervening natural amino acid, leucine. The unnatural fluorescent pentapeptide shows an excimer emission either via Förster resonance energy transfer (FRET) from the scaffold (ArTAA) acting as donor or via direct excitation of an acceptor chromophore, TPyAlaDo. Moreover, it serves as an effective fluorescence light-up probe for studying protein-peptide interaction. This is a new generation probe which would provide fundamental guidelines to design more of such conceptual fluorescent peptide-probe that would hold great promise for application in chemical biology.
51.●Regioselective
and Stereoselective Route to N2-β-Tetrazolyl Unnatural Nucleosides
via SN2 Reaction at the Anomeric Center of Hoffer’s
Chlorosugar● Bag,*
Subhendu Sekhar; Talukdar, Sangita; Anjali S.J.●
Bioorg. Med. Chem. Lett.
2016,
26(8), 2044-2050 Abstract: We are reporting a regioselective and stereospecific route to N2--tetrazolyl aromatic donor/acceptor unnatural nucleosides as new class of possible DNA base analogues. The SN2 substitution reaction at the anomeric center of Hoffer’s chlorosugar with various 5-substituted aromatic tetrazoles in THF in presence of K2CO3 proceeds with regioselectivity at N2-tetrazoes and stereospecificity at -chlorosugar with very good yield. The stereoelectronic and steric effects play a crucial role for the observed outcome which is also supported from a theoretical (DFT) study. The methodology is simple, eco-compatible and the tetrazolyl unnatural nucleosides might find applications in decorating DNA for various biotechnological and DNA based material science applications.
50.●Synthesis
of Functionalized Pyrazoles via Vanadium-Catalyzed C-N
Dehydrogenative Cross-Coupling and Fluorescence Switch-On Sensing of
BSA Protein● Sar,
Dinabandhu; Bag, Raghunath; Yashmeen, Afsana;
Bag,* Subhendu Sekhar;
Punniyamurthy,* Tharmalingam
●
Organic Letters,
2015,
17(21), 5308-5311.
Abstract: Vanadium-catalyzed C-N dehydrogenative cross-coupling of alkenyl hydrazones leading to functionalized pyrazoles is described in a 1:1 mixture of toluene : H2O using air as the terminal oxidant. The use of the commercial non-toxic VOSO4 as a recyclable catalyst, mild reaction conditions, scalability and the broad substrate scope are the significant practical features. Some of the product pyrazoles exhibit interesting photophysical properties. Fluorescence light-up sensing of BSA Protein by one of the pyrazole is also highlighted. 49.●Triazolo-β-Aza-ε-Amino Acid and Its Aromatic Analogue as Novel Scaffolds for β-turn Peptidomimetics● Bag, Subhendu Sekhar*; Jana, Subhashis; Yashmeen, Afsana; De, Suranjan● Chemical Communication, 2015, 51, 5242 (Emerging Investigators Issue).
48.●Wavelength Shifting Oligonucleotide Probe for the Detection of Adenosine of a Target DNA with Enhanced Fluorescence Signal● Bag, Subhendu Sekhar*; Pradhan, Manoj K.; Das, Suman K.; Jana, Subhashis; Bag, Raghunath● Bioorganic & Medicinal Chemistry Letters, 2014, 24, 4678.
47.●Design and Synthesis of Triazolyl-Donor/Acceptor Unnatural Nucleosides and Oligonucleotide Probes Containing Triazolyl-Phenanthrene Nucleoside●Bag, Subhendu Sekhar*; Talukdar, Sangita; Das, Suman Kalyan● Current Protocols in Nucleic Acids Chemistry 2014, 58:1.32.1-1.32.27.
46.●Dual Door Entry to Exciplex Emission in A Chimeric DNA Duplex Containing Non-nucleoside-Nucleoside Pair●Bag, Subhendu Sekhar*; Talukdar, Sangita; Kundu, Rajen; Saito, Isao; Jana, Subhashis● Chemical Communications 2014, 50, 829.
45.●Triazolyl-Donor/Acceptor Chromophore Decorated Unnatural Amino Acids and Peptides: FRET Event in β-Turn Conformation●Bag, Subhendu Sekhar*; Jana, Subhashis; Yashmeen Afsana; Senthilkumar, K; Bag, Raghunath● Chemical Communications 2014, 50, 433.
44.●Unnatural triazolyl nucleoside stabilizes an abasic site containing DNA duplex equally as the stabilization of a natural A-T pair●Bag, Subhendu Sekhar*; Kundu, Rajen; Sangita Talukdar ● RSC Advances 2013, 3, 21352.
43.●Sensing of micellar microenvironment with dual fluorescent probe, triazolylpyrene (TNDMBPy) ●Bag, Subhendu Sekhar*; Kundu, Rajen ● Journal of Fluorescence 2013, 23, 939-938.
42.●Triazolyl-Donor/Acceptor Sensing of biomolecules and label free discrimination of DNA containing a triple T-C/T-G mismatch pair with a fluorescence light-up probe, triazolylpyrene (TNDMBPy) ●Bag, Subhendu Sekhar*; Kundu, Rajen; Jana Subhashis ● Tetrahedron Lett. 2013, 54, 2627-2632.
41.●Solvatochromic fluorescent cyanophenoxazine: design, synthesis, photophysical properties and fluorescence light-up sensing of ct-DNA ●Bag, Subhendu Sekhar*; Ghorai, Samir; Jana, Subhashis; Mukherjee,* Chandan ● RSC Advances 2013, 3, 5374–5377.
40.●Triazolyl-Donor/Acceptor Chromophores Decorated Unnatural Nucleosides and Oligonucleotides with Duplex Stability Comparable to that of Natural A/T Pair ●Bag, Subhendu Sekhar*; Talukdar, Sangita; Matsumoto, Katsuhiko; Kundu, Rajen ● The Journal of Organic Chemistry 2013, 78, 278.
39.●WEB BASED COURSE-2● ● Bio-Organic Chemistry of Natural Enediyne Anticancer Antibiotics● Bag*, Subhendu Sekhar ● Under NPTEL Scheme. ●It contains 4 modules with 51 lectures. Website: http://nptel.iitm.ac.in/syllabus/syllabus.php?subjectId=104103068.
38.●WEB BASED COURSE-1● ●Bio-Organic Chemistry● Bag*, Subhendu Sekhar ● Under NPTEL Scheme. ●It contains 6 modules with 52 lectures. Website: http://www.nptel.iitm.ac.in/courses/104103018/.
37.●Highly
solvatochromic fluorescent naphthalimides: design, synthesis,
photophysical properties and fluorescence switch-on sensing of
ct-DNA
●Bag, Subhendu Sekhar*;
Pradhan, Manoj Kumar; Kundu, Rajen; Jana, Subhasish
● Bioorganic
& Medicinal Chemistry Letters,
2013,
23, 96-101.
36.● Expansion of the Genetic Alphabet: Unnatural Nucleobases and their Applications● Bag, Subhendu Sekhar;* Heemstra, Jennifer; Saito, Yoshio; Chenoweth, David M.● Journal of Nucleic Acids 2012, (Editorial Article), Article ID 718582, 2 pages, doi:10.1155/2012/718582. 35. ●Fluorometric sensing of Cu2+ ion with smart fluorescent light-up probe, triazolylpyrene (TNDMBPy)● Bag, Subhendu Sekhar*; Kundu Rajen; Talukdar Sangita● Tetrahedron Lett. 2012, 53, 5875-5879. Abstract: We report the detection of Cu2+ ion with fluorescence light-up probe, triazolylpyrene (TNDMBPy). Thus, the probe showed a remarkable fluorescence enhancement of both the monomer and excimer emissions and a 2:1 probe-Cu2+ complexation with high selectivity and stability constant. Our probe is also capable of sensing SDS micelle-encapsulated-Cu2+ ion in aqueous media proving its potential practical utility. Formation of excimer was also rationalized on the basis of DFT calculation.
34.●Synthesis and reactivity of enediyne-nucleobase hybrids: Effect of intramolecular π-stacking● Roy, Snigdha; Bag, Subhendu Sekhar; Basak, Amit● Tetrahedron 2012, 68, 8600-8611. Abstract: Three distinct classes of nucleobase-containing enediynes 1–9 with varying nature of the linker have been synthesized to explore the effect of π-stacking interaction in accelerating the rate of Bergman cyclization (BC). Chemical reactivity study, both experimental and computations demonstrated the important role that aromatic π-stacking interactions between the appended nucleobases within an enediyne frame play in lowering the activation barrier of Bergman cyclization.
33.●Click-Reagent Version of Sonogashira Coupling Protocol to Conjugated Fluorescent Alkynes with No or Reduced Homocoupling● Bag*, Subhendu Sekhar; Kundu, Rajen; Das, Manas● ChemInform 2011, 42 (26), no-no, DOI: 10.1002/chin.201126090. Abstract: The title reaction allows a highly efficient access to various diarylalkynes. 32.●Installation/Modulation of the Emission Response via Click Reaction● Bag, Subhendu Sekhar*; Kundu, Rajen● The Journal of Organic Chemistry 2011, 76(9), 3348-3356. Abstract: We have demonstrated the installation of a fluorescence property into a non-fluorescent precursor and modulation of an emission response of a pyrene fluorophore via click reaction. The synthesized fluorophores show different solvatochromicity and/or intramolecular charge transfer (ICT) feature as is revealed from the UV-visible, fluorescence photophysical properties of these fluorophores, and DFT/TDDFT calculation. We observed that some of the synthesized fluorophores showed purely ICT character while emission from some of them arose from LE state. A structure-less and solvent polarity-sensitive dual emission behavior was observed for one of the triazolyl-pyrene fluorophores that contains an electron donating –NMe2 substituent (fluorophore, 7a). Conversely, triazolyl-pyrene with an electron-withdrawing –CN group (fluorophore, 7b) showed a solvent polarity-independent vibronic emission. The effect of ICT on the photophysical properties of these fluorophores were studied by fluorescence emission spectra, and DFT/TDDFT calculations. Fluorescence life times were also measured in different solvents. All of our findings revealed the delicate interplay of structure and emission properties and thus having broader general utility. As the CT to LE intensity ratio can be employed as a sensing index, the dual emissive fluorophore can be utilized in designing molecular recognition system too. We envisage that our investigation is of importance for the development of new fluorophores with predetermined photophysical properties that may find a wide range of applications in chemistry, biology, and in material sciences.
31.●Click-Reagent Version of Sonogashira Coupling Protocol to Conjugated Fluorescent Alkynes with No or Reduced Homocoupling● Bag, Subhendu Sekhar*; Kundu, Rajen; Das, Manas● The Journal of Organic Chemistry Note 2011, 76(7), 2332-2337. Abstract: A click-reagent version of the Sonogashira-coupling protocol has been developed. Diarylalkynes with donor and/or acceptor substituents have been synthesized via this protocol at moderate to excellent yields and with no or drastically reduced quantities of undesired homocoupled side products. This protocol is green-solvent compatible, air-insensitive, and effective under microwave conditions.
30.●Selectivity in Garratt−Braverman Cyclization: An Experimental and Computational Study● Maji, Manasi; Mallick, Dibyendu; Mondal, Sayantan; Anoop, Anakuthil; Bag, Subhendu Sekhar; Basak, Amit; Jemmis, Eluvathingal D.● Organic Letters 2011, 13, 888-891. Abstract: Bispropargyl sulfones equipped with aromatic rings of dissimilar nature were synthesized. Under basic conditions, these sulfones isomerized to the bisallenic sulfones, creating a competitive scenario between two alternate Garratt-Braverman (GB) cyclization pathways. The observed product distribution ruled out the involvement of any ionic intermediate and supported the diradicalmechanismwith greater involvement of the electron-rich aromatic ring via the more nucleophilic radical. DFT-based calculations supported the diradical mechanism along with the observed selectivity.
29.●Singly and doubly labeled base-discriminating fluorescent oligonucleotide probes containing oxo-pyrene chromophore●Bag, Subhendu Sekhar*; Kundu, Rajen; Matsumoto, Katsuhiko; Saito,Yoshio; Saito, Isao● Bioorganic & Medidicinal Chemistry Letters 2010, 20, 3227-3230. Abstract: We have developed new oxo-pyrene labeled fluorescent nucleoside, Oxo-PyU which showed a strong fluorescence dependency on solvent polarity at long wavelength. The designed singly and doubly Oxo-PyU labeled fluorescent oligonucleotide probes were found highly efficient for the discrimination of A and consecutive AA bases of target DNA opposite to the labeled base via generation of enhanced fluorescence signal.
28.●Suppressed b-Effect of Silicon in 3-Silylated Monocyclic b-Lactams: The Role of Antiaromaticity● Bag, Subhendu Sekhar*; Kundu, Rajen; Basak, Amit; Slania, Zdenek● Organic Letters 2009, 11(24), 5722-5725. Abstract: The b-stabilizing effect of silicon substituent at C-3 on a C-4 cation and a radical in the 2-azetidinone systems is studied using NMR kinetics. While the b-effect is virtually nonexistent in the case of a cation, a foiled b-effect (only a 3-fold rate enhancement) is obsd. for a radical intermediate. From both the exptl. and theor. studies, it is demonstrated that antiaromaticity is playing the prime role in suppressing the b-stabilizing effect of silicon.
27.●A novel enediynyl peptide inhibitor of furin that blocks processing of proPDGF-A, B and proVEGF-C● Basak, Ajoy; Khatib, Abdel-Majid; Mohottalage, Dayani; Basak, Sarmistha; Kolajova, Maria; Bag, Subhendu Sekhar; Basak, Amit● PLoS One 2009, 4(11), No pp. Abstract: Background: Furin represents a crucial member of secretory mammalian subtilase, the Proprotein Convertase (PC) or Proprotein Convertase Subtilisin/Kexin (PCSK) superfamily. It has been linked to cancer, tumorgenesis, viral and bacterial pathogenesis. As a result it is considered a major target for intervention of these diseases. Methodol./Principal Findings: Herein, we report, for the first time, the synthesis and biol. evaluation of a newly designed potent furin inhibitor that contains a highly reactive beta-turn inducing and radical generating "enediynyl amino acid" (Eda) moiety. "Eda" was inserted between P1 and P1' residues of hfurin98-112 peptide, derived from the primary cleavage site of furin's own prodomain. The resulting hexadecapeptide deriv. inhibited furin in vitro with IC50 .apprx.40 nM when measured against the fluorogenic substrate Boc-RVRR-MCA. It also inhibited furin-mediated cleavage of a fluorogenic peptide derived from hSARS-CoV spike protein with IC50 .apprx.193 nM. Addnl. it also blocked furin-processing of growth factors proPDGF-A, B and VEGF-C that are linked to tumor genesis and cancer. CD study showed that this inhibitor displayed a predominantly beta-turn structure while western blots confirmed its ability to protect furin protein from self degrdn. Conclusion/Significance: These findings imply its potential as a therapeutic agent for intervention of cancer and other furin-assocd. diseases.
26.●Pyrene-labeled deoxyguanosine as a fluorescence sensor to discriminate single and double stranded DNA structures: Design of ends free molecular beacons● Matsumoto, Katsuhiko; Shinohara, Yuta; Bag, Subhendu Sekhar; Takeuchi, Yoshiki; Morii, Takashi; Saito, Yoshio; Saito Isao ● Bioorganic & Medicinal Chemistry Letters, 2009, 19, 6392-6395. Abstract: A novel fluorescent DNA probe containing pyrene-labeled C8 alkylamino-substituted 2′-deoxyguanosine was designed in order to discriminate single stranded and double stranded regions in DNA. This fluorescent sensor was used for the design of practically useful 3′- and 5′-ends free self-quenched molecular beacon (MB). Unique MB detectable by pyrene excimer fluorescence was also demonstrated.
25.●Fluorescence switching of photochromic vinylpyrene-substituted 2'-deoxyguanosine● Saito, Yoshio; Matsumoto, Katsuhiko; Takeuchi, Yoshiki; Bag, Subhendu Sekhar; Kodate, Satoshi; Morii, Takashi; Saito, Isao● Tetrahedron Letters 2009, 50(13), 1403-1406. Abstract: We synthesized C8-vinylpyrene-substituted 2'-deoxyguanosine and studied the photoregulated reversible E-Z isomerization. When E-isomer was irradiated with visible light (>420 nm), E- to Z-isomerization took place very rapidly, while upon irradn. with UV-light (.apprx.365 nm), Z-isomer was converted to E-isomer. When Z-isomer was illuminated with 365-400 nm light, no fluorescence was obsd., while E-isomer showed a very strong fluorescence emission, indicating that VPyG could be a useful fluorescence switching mol.
2006 - 2008
24.●Ends free and self-quenched molecular beacon with pyrene labeled pyrrolocytidine in the middle of the stem● Saito, Yoshio; Shinohara, Yuta; Bag, Subhendu Sekhar; Takeuchi, Yoshiki; Matsumoto, Katsuhiko; Saito, Isao● Tetrahedron 2009, 65(4), 934-939. Abstract: Pyrene labeled pyrrolocytidine was incorporated into an oligonucleotide to construct ends free and self-quenched mol. beacon in which the fluorophore contg. pyrrolocytidine was placed in the middle of the stem and used for the detection of a target DNA with an excellent efficiency.
23.●Design of an ultimate quencher free molecular beacon containing pyrrolocytidine-guanine base pair● Saito, Yoshio; Shinohara, Yuta; Bag, Subhendu Sekhar; Takeuchi, Yoshiki; Matsumoto, Katsuhiko; Saito, Isao● Nucleic Acids Symposium Series 2008, 52(1), 361-362. Abstract: A novel quencher free mol. beacon was designed in which fluorophore-labeled pyrrolocytidine was placed away from the stem terminal. This new type of MB was used for the detection of a target DNA with an excellent efficiency.
22.●Design of an efficient self-quenched molecular beacon for SNPs genotyping● Saito, Yoshio; Numajiri, Kyoko; Bag, Subhendu Sekhar; Mizuno, Erika; Saito, Isao. ●Nucleic Acids Symposium Series 2008, 52(1), 359-360. Abstract: Quencher free mol. beacon with an excellent signal to noise ratio was designed and used for SNPs genotyping.
21.●Fluorometric sensing of conformational switching of DNA; the use of fluorescence labeled C8-alkylamino substituted 2'-deoxyguanosine● Saito, Yoshio; Matsumoto, Katsuhiko; Bag, Subhendu Sekhar; Misawa, Akihiro; Saito, Isao● Nucleic Acids Symposium Series 2008, 52(1), 357-358. Abstract: C8-alkylamino substituted 2'-deoxyguanosine was incorporated into a DNA sequence and then labeled with pyrene. The conformational change from B- to Z-form was monitored using CD and fluorescence spectroscopy for both labeled and unlabeled ODNs.
20.●C8-alkynyl- and alkylamino substituted 2'-deoxyguanosines: a universal linker for nucleic acids modification● Saito, Yoshio; Matsumoto, Katsuhiko; Bag, Subhendu Sekhar; Ogasawara, Shinzi; Fujimoto, Kenzo; Hanawa, Kazuo; Saito, Isao● Tetrahedron 2008, 64(16), 3578-3588. Abstract: Incorporation of modified nucleosides with a flexible universal linker is of great value for post-synthetic modification of nucleic acids. Thus, C8-alkynyl- and alkylamino substituted 2'-deoxyguanosines I and II (x = 1,2,3,4) were synthesized for the first time and incorporated into short oligonucleotide sequences. The preference for syn conformation of these C8-substituted 2'-deoxyguanosines and the stability of the duplexes were discussed. The stabilizing effect of Z-DNA has also been examd.
19.●Synthesis of C8-alkylamino substituted 2'-deoxyguanosine● Saito, Yoshio; Matsumoto, Katsuhiko; Bag, Subhendu Sekhar; Ogasawara, Shinji; Suzuka, Isamu; Saito, Isao● Nucleic Acids Symposium Series 2007, (51), 147-148. Abstract: Synthesis of C8-alkynyl- and alkylamino substituted 2'-deoxyguanosine, e.g. I, is described. Protected alkynyl-amines are coupled with 8-bromo-2'-deoxyguanosine by a Pd(0)-mediate Sonogashira coupling protocol. Hydrogenation of alkynyl derivs. over 10% Pd/C under atm. pressure gave 8-alkylamino guanosine derivs. in nearly quant. yields.
18.●Design of dual-labeled oligonucleotide probes for SNPs genotyping● Saito, Yoshio; Bag, Subhendu Sekhar; Kodate, Satoshi; Suzuka, Isamu; Saito, Isao● Nucleic Acids Symposium Series 2007, (51), 23-24. Abstract: Our effort in designing base-discriminating fluorescence nucleosides (BDF), leads us to develop dual-labeled oligonucleotide probe in which the BDF nucleoside, PyU/2-AntU act as the donor sepd. by a defined base pair distance from the acceptor, fluorescein, attached to 5'-end of the probe. Thus, a longer wavelength emission from acceptor might allow the probe to be used for SNP typing in chip based detection technol. or in cell.
17.●Anthracene based base-discriminating fluorescent oligonucleotide probes for SNPs typing: Synthesis and photophysical properties● Saito, Yoshio; Motegi, Kaori; Bag, Subhendu Sekhar; Saito, Isao● Bioorganic & Medicinal Chemistry 2008, 16(1), 107-113. Abstract: 2- And 9-Anthracenecarboxamide labeled 2'-deoxyuridines were synthesized and their photophys. properties were examd. These oligonucleotide probes are capable of detecting adenine base on a target DNA sequence. It was also found that 2-anthracene based oligonucleotide probe is more efficient than the corresponding 9-anthracene based oligonucleotide in the application for DNA chip based SNP detection, due to its longer emission wavelength and high fluorescence intensity.
16.●Design of a novel G-quenched molecular beacon: A simple and efficient strategy for DNA sequence analysis● Saito, Yoshio; Mizuno, Erika; Bag, Subhendu Sekhar; Suzuka, Isamu; Saito, Isao● Chemical Communications 2007, (43), 4492-4494. (Highlited as Chemical Biology Research Article 2007, 12.) Abstract: G-quenched MBs are devised from readily available starting materials and used for sequence specific DNA detection with high efficiency.
15.●Synthesis and properties of acridone-labeled base-discriminating fluorescent (BDF) nucleosides● Saito, Yoshio; Hanawa, Kazuo; Bag, Subhendu Sekhar; Motegi, Kaori; Saito, Isao● Nucleic Acids Symposium Series 2006, (50), 181-182. Abstract: We have developed novel acridone-labeled BDF probe which showed its potential in recognizing opposite matched base from its target sequence via enhancement of fluorescence intensity. This probe emit at a longer wavelength than previously reported pyrene-labeled BDF probe and thus can be used in DNA chip.
14.●Synthesis of perylene-labeled base-discriminating fluorescent (BDF) nucleoside and its fluorescence properties● Bag, Subhendu Sekhar; Saito, Yoshio; Hanawa, Kazuo; Hayasi, Keigo; Kodate, Satoshi; Suzuka, Isamu; Saito, Isao● Nucleic Acids Symposium Series 2006, (50), 179-180. Abstract: We have synthesized perylene labeled BDF probe and its photophys. properties were explored. Perylene labeled oligonucleotide probe is capable of detecting cytosine from its target mismatch sequence by enhancement of fluorescence intensity.
13.●Dual-labeled oligonucleotide probe for sensing adenosine via FRET: A novel alternative to SNPs genotyping● Saito, Yoshio; Bag, Subhendu Sekhar; Kusakabe, Yuichi; Nagai, Chiharu; Matsumoto, Katsuhiko; Mizuno, Erika; Kodate, Satoshi; Suzuka, Isamu; Saito, Isao● Chemical Communications 2007, (21), 2133-2135. Abstract: A novel FRET based strategy for DNA sequence anal. utilizing base-discriminating fluorescence (BDF) nucleosides (PyU or 2-AntU) as donor in the dual-labeled oligonucleotide probe is reported. Emission from acceptor (5'-FAM) was obsd. upon excitation at the donor only when paired with adenine on the complementary target sequence.
12.●Highly selective fluorescent nucleobases for designing base-discriminating fluorescent probes● Saito, Isao; Saito, Yoshio; Hanawa, Kazuo; Hayashi, Keigo; Motegi, Kaori; Bag, Subhendu Sekhar; Dohno, Chikara; Ichiba, Tomohisa; Tainaka, Kazuki; Okamoto, Akimitsu● Pure and Applied Chemistry 2006, 78(12), 2305-2312. Abstract: There is increasing interest in single nucleotide polymorphism (SNP) typing since they can be used as markers to identify the genes that underlie complex diseases and to realize the full potential of pharmacogenomics in analyzing variable response to drugs. Among the different methodologies for SNP genotyping, the homogeneous assay is more amenable than the heterogeneous one. In this article, we will describe some of our most recently developed novel base-discriminating fluorescent (BDF) nucleosides useful for homogeneous SNP typing. Our novel concept led to the investigation of a new type of pyrene-labeled BDF nucleosides PyU, PyC, 8pyA, and MePydA, which emitted strong fluorescence only when the bases opposite the BDF bases are A, G, T, and C, resp. The DNA probes contg. four different BDF bases enabled us to distinguish single-base alterations by simply mixing with a sample soln. of target DNA. An example of SNP typing of c-Ha-ras SNP sequence has also been demonstrated. Detection of base insertion in insertion/deletion (indel) polymorphisms using pyrene excimer fluorescent probe has also been explored.
11.●Intelligent fluorescent nucleoside in sensing cytosine base: Importance of hydrophobic nature of perylene fluorophore● Bag, Subhendu Sekhar; Saito, Yoshio; Hanawa, Kazuo; Kodate, Satoshi; Suzuka, Isamu; Saito, Isao. ● Bioorganic & Medicinal Chemistry Letters 2006, 16(24), 6338-6341. Abstract: Fluorescence response upon hybridization of perylene labeled oligonucleotide probes depends on the microenvironment experienced by the perylene fluorophore. In mismatched duplex (PerU-C), enhanced fluorescence was obsd. while in matched duplex (PerU-A) fluorescence intensity decreased considerably. This observation will be a promising research effort in giving rise to a new powerful tool in detection of SNP.
10. ●Acridone-labeled base-discriminating fluorescence (BDF) nucleoside: synthesis and their photophysical properties● Saito, Yoshio; Hanawa, Kazuo; Kawasaki, Naomi; Bag, Subhendu Sekhar; Saito, Isao. ● Chemistry Letters 2006, 35(10), 1182-1183. Abstract: Acridone-labeled BDF bases AcA and AcU were incorporated into oligonucleotides (ODNs) and their photophys. properties were evaluated. The BDF probe containing AcA is extremely powerful in recognizing opposite base T via enhancement of the fluorescence intensity. Furthermore, they emit strong fluorescence at a longer wavelength than previously reported pyrene-labeled BDF probes and thus can be used for the detection of SNPs.
9. ●Design and synthesis of a novel enediynyl pentapeptide with predominantly b-turn structural motif and its potential as a fluorescence-based chemosensor● Basak, Amit; Bag, Subhendu Sekhar; Basak, Ajoy● Bioorganic & Medicinal Chemistry 2005, 13(12), 4096-4102. Abstract: A novel enediynyl pentapeptide in the protected form 1 was synthesized and characterized. It exists predominantly in b-turn structural motif as revealed by variable temperature. NMR and CD spectroscopy. In the presence of transition metal ions and gold nanoparticles, the fluorescence intensity of the peptide got enhanced with remarkable quantum yield with the Z-enediynyl w-amino acid acting as a fluorophoric reporter. The interesting photophysical behaviors with alkali and alkaline earth metal ions are also reported.
8. ●The effect of charge-transfer complexation/p-stacking interactions in lowering the activation barrier of the Bergman Cyclization● Basak, Amit; Bag, Subhendu Sekhar; Das, Amit K● European Journal of Organic Chemistry 2005, (7), 1239-1245. Abstract: To elaborate the concept of weak interactions and their effect on Bergman Cyclization (BC), several 1,2-dikynyl benzenes incorporating various combinations of donor and acceptor units in the two arms of the enediynes were designed and synthesized, and their charge-transfer interactions followed by UV/Vis spectroscopy. The thermal reactivities, as studied by DSC, show an increase in reactivity for the donor/acceptor or donor/donor combinations relative to the acceptor/acceptor pair. Such an increase in reactivity can be explained on the basis of intramol. charge transfer and p-stacking interactions between the two arms, which may lower the distance between the two acetylenic ends.
7. ●Purification, characterization and some studies on secondary structure of tannase from Aspergillus awamori Nakazawa● Mahapatra, Kalyani; Nanda, Ranjan Kumar; Bag, Subhendu Sekhar; Banerjee, Rintu; Pandey, Ashok; Szakacs, George● Process Biochemistry (Oxford, United Kingdom) 2005, 40(10), 3251-3254. Abstract: Tannase (EC 3.1.1.20) (I) of A. awamori Nakazawa was purified and characterized. Optimal conditions of prodn. were detd. using varying substrate combinations and studying fermn. on various media combinations. Fermn. was carried out for 46 h for optimum enzyme prodn. Enzyme samples were obtained from the broth after fermn. by acetone pptn. of the supernatant followed by gel filtration chromatog. The properties of purified I were investigated. The optimum temp. and pH were investigated and the effects of urea, surfactants, and chelators were studied. I from this new isolate exhibited optimum activity at 35 and pH 5.0. Urea concns. of >3M were inhibitory. Increasing concns. of sodium lauryl sulfate (SLS) also led to a decrease in activity, with 2% SLS being inhibitory. Increasing concns. of EDTA also had an inhibitory effect on I. I was found to be a glycoprotein. CD anal. of purified fractions of I indicated that the .beta.-sheet structure was predominant indicating its globular nature.
6. ●Effect of Remote Trigonal Carbons on the Kinetics of Bergman Cyclization: Synthesis and Chemical Reactivity of Pyridazinedione-Based Enediynes● Basak, Amit; Bag, Subhendu Sekhar; Majumder, Pooja Anjali; Das, Amit Kumar; Bertolasi, Valerio● Journal of Organic Chemistry 2004, 69(20), 6927-6930. Abstract: The synthesis and chem. reactivity of pyridazinedione-based enediynes (1, 2) are described. Both of these enediynes, namely the dihydro compd. 1 and its corresponding tetrahydro analog 2, were prepd. by double N,O-alkylation of the corresponding heterocyclic system with the acyclic enediynyl dibromide 8 in good yields. Their single-crystal X-ray structures revealed similar c, d distances (distance between the acetylenic carbons undergoing covalent connection in Bergman cyclization). Interestingly, these mols. undergo Bergman cyclization at different rates, and the reactivity is shown to be dependent upon the state of hybridization of C-4 and C-5 atoms of the parent heterocyclic ring.
5. ●Molecular recognition in b-lactams: The crystal packing in 4-sulfonyl b -lactams● Basak, Amit; Bag, Subhendu Sekhar; Mazumdar, Pooja Anjali; Bertolasi, Valerio; Das, Amit Kumar● Journal of Chemical Research 2004, (5), 318-321. Abstract: Single crystal x-ray structures of 4-Ph sulfonyl 2-azetidinone 1, a 1:2 conglomerate of the corresponding 3-Me (trans) and 3,3-di-Me derivs., and 3-acetoxymethyl 1,4-di-Ph 2-azetidinone revealed interesting variation in crystal packing dictated by H-bonding and hydrophobic interactions which may be responsible for mol. recognition in b-lactams.
4. ●Synthesis and reactivity of enediynyl amino acids and peptides: a novel concept in lowering the activation energy of Bergman cyclisation by H-bonding and electrostatic interactions● Basak Amit; Bag, Subhendu Sekhar; Bdour Hussam M. M. Chemical communications 2003, (20), 2614-5. Abstract: Novel enediynyl amino acids and peptides 3 and 5-8 were synthesized and their thermal reactivity towards Bergman cyclization studied and compared with the earlier reported amino acid 4, which demonstrated, for the first time, the effect of H-bonding and electrostatic interactions in lowering the activation energy of Bergman cyclization.
3. ●Chelation-Controlled Bergman Cyclization: Synthesis and Reactivity of Enediynyl Ligands ● Basak, Amit; Mandal, Subrata; Bag, Subhendu Sekhar● Chemical Reviews 2003, 103(10), 4077-4094. Abstract: A review with 150 references.
2. ●Synthesis, reactivity and conformational preferences of novel enediynyl peptides: a possible scaffold for b-sheet capping turns● Basak, Amit; Rudra, Kakali Rani; Bag, Subhendu Sekhar; Basak, Ajoy● Journal of the Chemical Society, Perkin Transactions 1 2002, (15), 1805-1809. Abstract: Novel enediynyl tripeptides 2(a-c) in fully protected forms have been prepd. via a sequence of palladium(0)-based Sonogashira coupling. The thermal reactivity of these peptides was shown to be dependent upon the nature of the side chain in the amino acids. Anal. of the CD-spectra of these peptides as well as the variation of chem. shifts with temp. revealed the presence of a b-sheet nucleating conformation in equil. with a conformation induced by H-bond formation between the CO and NH belonging to the enediynyl amino acid.
1. ●Diastereoselective synthesis of 4-substituted L-prolines by intramolecular radical cyclization of N-aryl sulphonyl-N-allyl 3-bromoalanines: interesting dependence of selectivity on the nature of sulphonamido groups● Basak, Amit; Bag, Subhendu Sekhar; Rudra, Kakali Rani; Barman, Jharna; Dutta, Sumana.● Chemistry Letters 2002, 7, 710-711. Abstract: Enantiopure 4-substituted L-proline derivs. have been prepd. via intramol. radical cyclization of N-aryl sulfonyl-N-allyl-3-bromo-L-alanines in high yields. Surprisingly, the extent of selectivity was found to be primarily dependent on the nature of sulfonamido aryl group and could be as high as 33:1 using naphthyl sulfonamide.
Under Preparation/Communicated
Conference Paper 1.●87th Canadian Chemistry Conference and Exhibition, LCC-Ballrooms, Canada (2004), Poster BMP-00483: ●“A beta-Turn Inducing Enediyne Amino Acid Scaffold for Developing Inhibitors of Proprotein Convertase Furin”●
2.●XXXIst IUPAC Conference on Photochemistry 2006, conducted by IUPAC; held on 2-7th April, 2006, at Kyoto University; Japan. Topic of the Paper: ●“Highly Selective Fluorescent Nucleobases for Designing Base-Discriminating Fluorescence Probe”●
3.●The 33rd Symposium on Nucleic Acids Chemistry (SNAC) held on 20-22, November, 2006, at Osaka University, Japan. Topic of the Papers: ●(a) “Synthesis of perylene-labeled base-discriminating fluorescent (BDF) nucleoside and its fluorescence properties”. ●(b) “Synthesis and properties of acridone-labeled base-discriminating fluorescent (BDF) nucleosides”●
4.●KAKENHI International Symposium on Molecular Nanodynamics, held on July 1-3, 2006 at Osaka University, Japan. Topic of the Poster: ●“Role of Hydrophobicity in Sensing Mismatched Base Cytosine by Perylene Labelled Oligonucleotide Probe”●
5.●41st IUPAC World Chemistry Congress on “Chemistry Protecting Health, Natural Environment, and Cultural Heritage” held on August 5-10, 2007, at Torino, Italy, Poster presented ●“Design and synthesis of base-discriminating fluorescent (BDF) oligonucleotide probe: A novel alternative for genotyping SNPs”● 6.●5th International Symposium on Nucleic Acids Chemistry (SNAC2007) held on November 20-22, 2007 at Tokyo University, Japan. Oral presentation ●“Design of dual-labeled oligonucleotide probes for SNPs genotyping”●
7.●XXIst IUPAC International Conference on Photochemistry 2008, conducted by IUPAC; held on 28th July-1st August, 2008 at Goteborg; Sweden. Topic of the Paper presented: ●“Design of G-quenched molecular beacons for DNA detection”●
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