Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1399056 | European Journal of Medicinal Chemistry | 2013 | 9 Pages |
•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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