Neha Tripathi - Academia.edu (original) (raw)
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CSIR-North East Institute of Science and Technology
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Papers by Neha Tripathi
ACS Medicinal Chemistry Letters, 2015
A study of structure-based modulation of known ligands of hTopoIIα, an important enzyme involved ... more A study of structure-based modulation of known ligands of hTopoIIα, an important enzyme involved in DNA processes, coupled with synthesis and in vitro assays led to the establishment of a strategy of rational switch in mode of inhibition of the enzyme's catalytic cycle. 6-Arylated derivatives of known imidazopyridine ligands were found to be selective inhibitors of hTopoIIα, while not showing TopoI inhibition and DNA binding. Interestingly, while the parent imidazopyridines acted as ATP-competitive inhibitors, arylated derivatives inhibited DNA cleavage similar to merbarone, indicating a switch in mode of inhibition from ATP-hydrolysis to the DNA-cleavage stage of catalytic cycle of the enzyme. The 6-aryl-imidazopyridines were relatively more cytotoxic than etoposide in cancer cells and less toxic to normal cells. Such unprecedented strategy will encourage research on "choicebased change" in target-specific mode of action for rapid drug discovery.
Med. Chem. Commun., 2014
Novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines that exhibit potent tubulin polymerization i... more Novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines that exhibit potent tubulin polymerization inhibition, anticancer activity, anti-migration of cancer cells, chromosomal damage, and apoptosis have been developed.
ACS Medicinal Chemistry Letters, 2015
A study of structure-based modulation of known ligands of hTopoIIα, an important enzyme involved ... more A study of structure-based modulation of known ligands of hTopoIIα, an important enzyme involved in DNA processes, coupled with synthesis and in vitro assays led to the establishment of a strategy of rational switch in mode of inhibition of the enzyme's catalytic cycle. 6-Arylated derivatives of known imidazopyridine ligands were found to be selective inhibitors of hTopoIIα, while not showing TopoI inhibition and DNA binding. Interestingly, while the parent imidazopyridines acted as ATP-competitive inhibitors, arylated derivatives inhibited DNA cleavage similar to merbarone, indicating a switch in mode of inhibition from ATP-hydrolysis to the DNA-cleavage stage of catalytic cycle of the enzyme. The 6-aryl-imidazopyridines were relatively more cytotoxic than etoposide in cancer cells and less toxic to normal cells. Such unprecedented strategy will encourage research on "choicebased change" in target-specific mode of action for rapid drug discovery.
Med. Chem. Commun., 2014
Novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines that exhibit potent tubulin polymerization i... more Novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines that exhibit potent tubulin polymerization inhibition, anticancer activity, anti-migration of cancer cells, chromosomal damage, and apoptosis have been developed.