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
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
收藏
页码:630 / 645
页数:16
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