Syntheses and potential anti-prostate cancer activities of ionone-based chalcones.

Abstract

We report the SAR studies of 43 ionone-based chalcones that demonstrate substantial in vitro anti-proliferative activities in LNCaP, MDA-PCa-2b, 22Rv1, C4-2B and PC-3 prostate cancer cell lines. Compound 25 with an IC(50) value of 0.74 microM in LNCaP cells potently antagonizes DHT-induced transactivation of the wild type and the clinically relevant T877A, W741C and H874Y mutated androgen receptors, representing a novel chalcone as pan-antagonist of androgen receptor.

• Authors: Jinming Zhou, Guoyan Geng, Gerald Batist, Jian Hui Wu
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 4 Pg. 1183-6 (Feb 15 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19138519 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Androgen Receptor Antagonists
• Antineoplastic Agents
• Chalcones
• Norisoprenoids
• Receptors, Androgen

Topics

• Androgen Receptor Antagonists
• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Chalcones (chemical synthesis, chemistry, pharmacology)
• Combinatorial Chemistry Techniques
• Drug Screening Assays, Antitumor
• Humans
• Male
• Mice
• Molecular Structure
• Mutation
• Norisoprenoids (chemical synthesis, chemistry, pharmacology)
• Prostatic Neoplasms (drug therapy)
• Receptors, Androgen (genetics)
• Structure-Activity Relationship