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

• A series of pyrimidine bearing thiazolidin-4-one were designed and synthesized under microwave irradiation.
• Initial screening of compounds showed remarkable to good anticancer activity by NCI panel.
• Compound 2 exhibited significant growth inhibition and was further screened at five dose level.
• Compound 2 could be used as a lead compound for developing new potential anticancer agents.

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 μM) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI50 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.

A series of new pyrimidine molecules bearing thiazolidin-4-one were synthesized under microwave irradiation from 4-(2-chlorophenyl)-6-(2,4-dichloro phenyl)pyrimidin-2-amine for getting promising anticancer agents at NCI against full NCI 60 cell lines panel. The present study may result in the development of new anticancer agents in the near future.Figure optionsDownload as PowerPoint slide