Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents

被引：37

作者：

Rashid, Mohd ^{[1
]}

Husain, Asif ^{[1
]}

Shaharyar, Mohammad ^{[1
]}

Mishra, Ravinesh ^{[1
]}

Hussain, Afzal ^{[1
]}

Afzal, Obaid ^{[1
]}

机构：

[1] Jamie Hamdard Hamdard Univ, Dept Pharmaceut Chem, Fac Pharm, New Delhi 110062, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 83卷

关键词：

In-vitro anticancer activity; NCI 60 cell line; CDK; 2; enzyme; Thiazolidin-4-one; NATIONAL-CANCER-INSTITUTE; CYCLIN-DEPENDENT KINASES; TRIAZOLO-THIADIAZOLES; BEARING OXADIAZOLE; DRUG DISCOVERY; DERIVATIVES; INHIBITORS; ANTIBACTERIAL; CHEMOTHERAPY; OLOMOUCINE;

D O I：

10.1016/j.ejmech.2014.06.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2-amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 mu M) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 mu M). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI(50) 0.52) and no cytotoxicity seen (LC50 > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：630 / 645

页数：16

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