Medicinal Chemistry

Synthesis and In Vitro Antiproliferative Evaluation of Some B-norcholesteryl thiazole Derivatives

Abstract

Yanmin Huang, Binbin Qi, Jianguo Cui, Zhipin Liu, Chunfang Gan, Dandan Zhao, Qifu Lin and Haixin Shi

Some novel B-norcholesteryl thiazole derivatives were synthesized and their structures were characterized by IR, NMR and HRMS. The antiproliferative activity of the compounds against human cervical carcinoma(HeLa), human lung carcinoma (A549), human liver carcinoma (HEPG2) and normal kidney epithelial (HEK293T) cells was assayed. The results revealed that compounds 14 and 17 with a structure of N-methylthiazole showed distinct antiproliferative activity against A549 and HEPG2 cells. Compounds 20-24 with a structure of N-phenylthiazole displayed a selective antiproliferativeactivity on HeLa cells and were almost inactive to normal kidney epithelial cells (HEK293T). The research provided a theoretical reference for the exploration of new anti-cancer agents and may be useful for the design of novel chemotherapeutic drugs.