Synthesis of Dehydroepiandrosteronyl Thiazole Derivatives and Their Antiproliferative Evaluation

Using dehydroepiandrosterone as starting material, 16 dehydroepiandrosteronyl thiazol derivatives with different structures had been synthesized via microwave irradiation assisted one-pot reaction and general synthetic method, and their structures were characterized by IR, NMR and HRMS. The antiproliferative activity of the compounds was evaluated against human cervical carcinoma (HeLa), human lung carcinoma (A549), human liver carcinoma cells (HEPG2) and normal kidney epithelial cells (HEK293T). The results showed that compound 4 displayed significant inhibitory activity to tested cancer cells, and the values of IC50 were 13.2, 11.3 and 8.3 μmol•L -1 respectively, but was almost inactive to HEK293T cells (IC50>100 μmol•L ). However, other compounds did not exhibit distinct antiproliferative activity to all tested cells.