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Eur J Med Chem ; 54: 952-8, 2012 Aug.
Article in English | MEDLINE | ID: mdl-22789812

ABSTRACT

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 (IC(50) 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) (IC(50) 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.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Flavonols/chemical synthesis , Flavonols/pharmacology , Prostatic Neoplasms/pathology , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacokinetics , Biological Availability , Cell Line, Tumor , Chemistry Techniques, Synthetic , Drug Stability , Flavonols/chemistry , Flavonols/pharmacokinetics , Humans , Hydrophobic and Hydrophilic Interactions , Male
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