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

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Title Statement <p>Design, synthesis of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1<em>H</em>)-one derivatives and evaluation of their <em>in vitro </em>tyrosine kinase inhibitor activity</p>
 
Added Entry - Uncontrolled Name Fonseca, Viveka ; Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa 403 401, India
Chandavarkar, Sachin Kishore; Department of Pharmacognosy, ASPM College of Pharmacy, Sangulwadi 416 810, India
Dabholkar, Renuka ; Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa 403 401, India
Dessai, Prachita Gauns; Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa 403 401, India
Deshpande, Mangirish ; Department of Pharmacology, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa 403 401, India
Desai, Shivalingrao N Mamle; Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa 403 401, India
 
Uncontrolled Index Term Quinolin-2-one, anticancer, MDA-MB cell line, Molegro Virtual Docker, EGFRK protein
 
Summary, etc. <p class="Abstract">The present investigation deals with molecular docking, synthesis, characterization, and evaluation of <em>in vitro </em>tyrosine kinase inhibitor activity of a series of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-<br /> 3,4-dihydroquinolin-2(1<em>H</em>)-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, <sup>1</sup>H NMR and <sup>13</sup>C NMR and mass spectral data). Twelve derivatives were tested for their <em>in vitro </em>tyrosine kinase inhibitor activity using MDA-MB cell line. Compound 4-[2-(4-bromophenyl)hydrazono]-3-(1-hydroxyethyl)-1- methyl-<br /> 3,4-dihydroquinolin-2(1<em>H</em>)-one (III-b4) was found to be the most cytotoxic compound as compared to other synthesized derivatives, with IC<sub>50</sub> value of 0.0515 μM against MDA- MB cell line.</p><p> </p>
 
Publication, Distribution, Etc. Indian Journal of Chemistry -Section B (IJC-B)
2021-02-15 15:57:41
 
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http://op.niscair.res.in/index.php/IJCB/article/view/32682
 
Data Source Entry Indian Journal of Chemistry -Section B (IJC-B); ##issue.vol## 60, ##issue.no## 2 (2021): Indian Journal of Chemistry Section - B (IJCB)
 
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Nonspecific Relationship Entry http://op.niscair.res.in/index.php/IJCB/article/download/32682/465501378
http://op.niscair.res.in/index.php/IJCB/article/download/32682/0
http://op.niscair.res.in/index.php/IJCB/article/download/32682/0
http://op.niscair.res.in/index.php/IJCB/article/download/32682/0
 
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