Synthesis and cytotoxic activity of some novel steroidal C-17 pyrazolinyl derivatives.

Abstract Fourteen novel steroidal C-17 pyrazolinyl derivatives 9a – g and 10a – g were synthesized from commercially available progesterone and tested for their cytotoxic activity against brine shrimp ( Artemia salina ) and three human cancer cell lines (NCI-H460, HeLa, and HepG2). Some of these synthetic compounds exhibited significant cytotoxic activity, and treatment of HeLa cells with compound 10b resulted in the cell population arrest in the S phase. A structure–activity relationship was discussed.