16α-HETEROARYL PREGNENOLONE ACETATE AND A PROCESS FOR PREPARATION THEREOF

摘要

The present invention relates to microwave assisted facile Michael addition of benzimidazole and imidazole to steroidal α,β-unsaturated ketones under solvent-free condition to afford corresponding Michael adducts 16α-(1H-benzimidazol-1-yl)-pregnenolone acetate (1) and 16α-(1H-imidazol-1-yl)-pregnenolone acetate (2). Compound 1 showed in vitro cytotoxic activities almost comparable to the drug doxorubicin against cervical HeLa cancer cell line (compound 1, IC50 = 8.3317, doxorubicin IC50 = 7.8126), prostate DU 205 cancer cell line (compound 1, IC50 = 12.0192, doxorubicin IC50 = 9.1194) and breast cancer MCF-7 cell line (compound 1, IC50 = 8.2855, doxorubicin IC50 = 7.5094).