Synthesis and in vitro antineoplastic evaluation of certain 16-(4-substituted benzylidene) derivatives of androst-5-ene.

Abstract

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.

• Authors: Sonal Dubey, Poonam Piplani, Dharam Paul Jindal
• Journal: Chemistry & biodiversity (Chem Biodivers) Vol. 1 Issue 10 Pg. 1529-36 (Oct 2004) ISSN: 1612-1880 [Electronic] Switzerland
• PMID: 17191796 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Androstenols
• Antineoplastic Agents
• Benzylidene Compounds
• androst-5-en-3-ol

Topics

• Androstenols (chemical synthesis, pharmacology)
• Antineoplastic Agents (chemical synthesis, pharmacology)
• Benzylidene Compounds (chemical synthesis, pharmacology)
• Cell Line, Tumor
• Drug Screening Assays, Antitumor (methods)
• Humans