2. Academic Validation
  3. Syntheses and potential anti-prostate cancer activities of ionone-based chalcones

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

  • Bioorg Med Chem Lett. 2009 Feb 15;19(4):1183-6. doi: 10.1016/j.bmcl.2008.12.089.
Jinming Zhou 1,  Guoyan Geng,  Gerald Batist,  Jian Hui Wu
Affiliations

Affiliation

  • 1 Department of Oncology, McGill University, Montreal, Canada.
PMID: 19138519 DOI: 10.1016/j.bmcl.2008.12.089
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.

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