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

作者：Rashid Mohd; Husain Asif^*; Shaharyar Mohammad; Mishra Ravinesh; Hussain Afzal; Afzal Obaid

来源：European Journal of Medicinal Chemistry, 2014, 83: 630-645.

DOI：10.1016/j.ejmech.2014.06.033

• In-vitro anticancer activity
• NCI 60 cell line
• CDK 2 enzyme
• Thiazolidin-4-one

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.

• 出版日期2014-8-18