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

• 14 novel steroidal C-17 pyrazolinyl analogs were prepared.
• Cytotoxic activities were dependent on level of aromatic ring substitution.
• Several compounds showed marked cytotoxic effects.
• Influence of cell cycle by 10b was investigated.

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.

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