Syntheses and potential anti-prostate cancer activities of ionone-based chalcones
Syntheses and potential anti-prostate cancer activities of ionone-based chalcones
- Bioorganic & Medicinal Chemistry Letters, 19(4), p.1183-1186, 2009 .
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 IC50 value of 0.74 lM 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.
ANDROGEN RECEPTOR
MUTATION
ANTIANDROGEN
PAN-ANTAGONIST
IONONE DERIVATIVES
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 IC50 value of 0.74 lM 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.
ANDROGEN RECEPTOR
MUTATION
ANTIANDROGEN
PAN-ANTAGONIST
IONONE DERIVATIVES