Synthesis and in vitro antineoplastic evaluation of certain 16-(4-substituted benzylidene) derivatives of androst-5-ene.
In a systematic effort aimed at identifying new steroidal cytotoxic agents with potent antiproliferative activity against cancer cells, we synthesized certain 16-[4-(NO2, CN, and i-Pr)substituted]benzylidene derivatives of androst-5-ene, 7-25, with pyrrolidino functionality in the 3beta-position of the steroid nucleus, i.e., 13-18 and 25. The selected compounds were examined for their cytotoxicity against a panel of three human cancer cell lines at the National Cancer Institute (NCI), Bethesda, USA. The results presented herein provide experimental evidence that compounds 7, 9, 10, 12, 16, and 19-21 induced apoptosis in human cancer cells.
Dubey
Sonal
S
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014 India.
Piplani
Poonam
P
Jindal
Dharam Paul
DP
D000737:Androstenols / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans
D000737:Androstenols; D000970:Antineoplastic Agents; D001597:Benzylidene Compounds; C034744:androst-5-en-3-ol