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Design, synthesis of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives and evaluation of their in vitro tyrosine kinase inhibitor activity

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Title Design, synthesis of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives and evaluation of their in vitro tyrosine kinase inhibitor activity
 
Creator Fonseca, Viveka
Chandavarkar, Sachin
Dabholkar, Renuka
Dessai, Prachita Gauns
Deshpande, Mangirish
Desai, Shivalingrao N Mamle
 
Subject Quinolin-2-one
Anticancer
MDA-MB cell line
Molegro Virtual Docker
EGFRK protein
 
Description 267-272
The present investigation deals with molecular docking, synthesis, characterization, and evaluation of in vitro tyrosine kinase inhibitor activity of a series of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives {III-a(1-12)/III-b(1-12)}. Molecular docking studies of the title compounds were carried out using Molegro Virtual Docker (MVD-2013, 6.0) software. The MolDock scores of the derivatives ranged from (−66.508) to (−101.274); whereas the MolDock score of standard 4-anilinoquinazoline ligand was found to be (−105.219). Most of the synthesized qunolin-2-one derivatives showed better affinity towards EGFRK protein as compared to standard drug imatinib (−104.253). All the synthesized compounds were satisfactorily characterized by physical and spectral analysis (UV, IR, 1H NMR and 13C NMR and mass spectral data). Twelve derivatives were tested for their in vitro tyrosine kinase inhibitor activity using MDA-MB cell line. Compound 4-[2-(4-bromophenyl)hydrazono]-3-(1-hydroxyethyl)-1- methyl- 3,4-dihydroquinolin-2(1H)-one (III-b4) was found to be the most cytotoxic compound as compared to other synthesized derivatives, with IC50 value of 0.0515 μM against MDA- MB cell line.
 
Date 2021-02-11T10:30:42Z
2021-02-11T10:30:42Z
2021-02
 
Type Article
 
Identifier 0975-0983(Online); 0376-4699(Print)
http://nopr.niscair.res.in/handle/123456789/56214
 
Language en_US
 
Rights CC Attribution-Noncommercial-No Derivative Works 2.5 India
 
Publisher NISCAIR-CSIR, India
 
Source IJC-B Vol.60B(02) [February 2021]