Structure-activity relationship and pharmacokinetic studies of 3-O-substitutedflavonols as anti-prostate cancer agents.

ABSTRACT: Thirty-eight 3-O-substituted-3',4'-dimethoxyflavonols and twenty-five 3-O-substituted-3',4',7-trimethoxyflavonols have been synthesized for systematic investigation on the structure-activity relationships of 3-O-substituted-3',4'-dimethoxyflavonols in three human prostate cancer cell models. Our findings indicate that incorporation of an appropriate amino group to 3-OH of 3',4'-dimethoxyflavonol and 3',4',7-trimethoxyflavonol through a 3- to 5-carbon linker can substantially improve the in vitro antiproliferative potency in three human prostate cancer cell models, but not in two non-neoplastic human epithelial cell models (MCF 10A and PWR-1E). 1-Methylpiperazine, pyrrolidine, and dibutylamine are optimal terminal amine groups that, in combination with a 3- to 5-carbon linker, are notably b

SUBMITTER: Li X 

PROVIDER: S-EPMC6245954 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature