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Your search keyword '"Kotresha, D."' showing total 2 results
Start Over Author "Kotresha, D." Publisher elsevier science
2 results on '"Kotresha, D."'

1. Spirooxindole-pyrrolidine heterocyclic hybrids promotes apoptosis through activation of caspase-3.

Author

Kumar RS, Almansour AI, Arumugam N, Mohammad F, Kotresha D, and Menéndez JC

Subjects
Antineoplastic Agents chemistry, Cell Line, Tumor, Cell Proliferation drug effects, Cycloaddition Reaction, Humans, Spiro Compounds chemistry, Structure-Activity Relationship, Antineoplastic Agents pharmacology, Apoptosis drug effects, Caspase 3 metabolism, Indoles chemistry, Pyrrolidines chemistry
Abstract

A small library of spirooxindole-pyrrolidine hybrids have been synthesized for the first time in an ionic liquid, [bmim]Br in good to excellent yields employing a new class of non-stabilized azomethine ylides derived from isatin and tyrosine, a combination that has been rarely employed for the in situ generation of azomethine ylides using [3+2] cycloaddition strategy. Following the synthesis and characterization of the spirooxindole-pyrrolidine heterocyclic hybrids, they were tested for their anticancer activity as against the changes in the concentrations and time periods with different in vitro cell cultures containing cancer and non-cancer cells, where the results revealed for a potential therapeutic activity. Further analysis for the mechanism of cell death by the cancer cells indicated for the caspase-dependent apoptotic pathway, specifically mediated by caspase-3. Based on these results, it can be demonstrated that the synthesized spirooxindole-pyrrolidine hybrids may serve as one of the better therapeutic agents used for the treatment of malignant tumors., (Copyright © 2019 Elsevier Ltd. All rights reserved.)

Published
2019
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2. Dispiropyrrolidinyl-piperidone embedded indeno[1,2-b]quinoxaline heterocyclic hybrids: Synthesis, cholinesterase inhibitory activity and their molecular docking simulation.

Author

Arumugam N, Almansour AI, Kumar RS, Kotresha D, Saiswaroop R, and Venketesh S

Subjects
Acetylcholinesterase chemistry, Binding Sites, Butyrylcholinesterase chemistry, Catalytic Domain, Cholinesterase Inhibitors metabolism, Cholinesterase Inhibitors pharmacokinetics, Half-Life, Humans, Inhibitory Concentration 50, Solubility, Acetylcholinesterase metabolism, Butyrylcholinesterase metabolism, Cholinesterase Inhibitors chemical synthesis, Molecular Docking Simulation, Piperidones chemistry, Quinoxalines chemistry
Abstract

A small library of new class of dispiropyrrolidinyl-piperidone tethered indono[1,2-b]quinoxaline heterocyclic hybrids 7a-j were synthesized employing multicomponent 1,3-dipolar cycloaddition strategy in [bmim]Br. The azomethine ylide employed is first of its kind and generated in situ from indenoquinoxalinone and l-tryptophan, a combination that has not been employed previously for the in situ generation of azomethine ylides. The synthesized heterocyclic hybrids 7a-j were evaluated for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, therein compounds 7h and 7j displayed more potent AChE and BChE enzyme inhibition than the standard drug with IC 50 values of 3.22, 2.01, 12.40 and 10.45 mM, respectively. Molecular docking studies have also been investigated for most active compounds that disclosed interesting binding templates to the active site channel of cholinesterase enzyme., (Copyright © 2019 Elsevier Ltd. All rights reserved.)

Published
2019
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