A library of flavonol analogues was synthesised and evaluated as potential anticancer agents against a human prostate cancer cell line, 22rν1.
Compounds 3, 8 and 11 (IC50 2.6, 3.3 and 4.0 μM respectively) showed potent cancer cell growth inhibition, comparable to the lead compound 3',4',5'-trimethoxyflavonol (1) (IC50 3.1 μM) and superior to the naturally occurring flavonols quercetin (16) and fisetin (22) (both >15 μM). Results indicate that the 3',4',5'- arrangement of either hydroxy (OH) or methoxy (OMe) residues is important for growth arrest of these cells and that the OMe analogues may be superior to their OH counterparts. Compounds 1, 3, 8 and 11 warrant further investigation as potential agents for the management of prostate cancer.
Written by:
Britton RG, Horner-Glister E, Pomenya OA, Smith EE, Denton R, Jenkins PR, Steward WP, Brown K, Gescher A, Sale S. Are you the author?
Department of Cancer Studies and Molecular Medicine, George Porter Building, University of Leicester, Leicester LE1 7RH, UK.
Reference: Eur J Med Chem. 2012 Aug;54:952-8.
doi: 10.1016/j.ejmech.2012.06.031
PubMed Abstract
PMID: 22789812
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