1394018-27-9Relevant academic research and scientific papers
3-O-Substituted-3',4',5'-trimethoxyflavonols: Synthesis and cell-based evaluation as anti-prostate cancer agents
Li, Xiang,Lee, Maizie,Chen, Guanglin,Zhang, Qiang,Zheng, Shilong,Wang, Guangdi,Chen, Qiao-Hong
, (2017)
Twenty-two 3-O-substituted-3',4',5'-trimethoxyflavonols have been designed and synthesized for their anti-proliferative activity towards three human prostate cancer cell lines. Our results indicate that most of them are significantly more potent than the parent 3',4',5'-trimethoxyflavonol in inhibiting the cell proliferation in PC-3 and LNCaP prostate cancer cell models. 3-O-Substituted-3',4',5'-trimethoxyflavonols have generally higher potency towards PC-3 and LNCaP cell lines than the DU145 cell line. Incorporation of an ethyl group to 3-OH of 3',4',5'-trimethoxyflavonol leads to 3-O-ethyl-3',4',5'-trimethoxyflavonol as the optimal derivative with up to 36-fold enhanced potency as compared with the corresponding lead compound 3',4',5'-trimethoxyflavonol, but with reversed PC-3 cell apoptotic response. Introduction of a dipentylaminopropyl group to 3-OH increases not only the antiproliferative potency but also the ability in activating PC-3 cell apoptosis. Our findings imply that modification on 3-OH of trimethoxyflavonol can further enhance its in vitro anti-proliferative potency and PC-3 cell apoptosis induction.
Synthesis and biological evaluation of novel flavonols as potential anti-prostate cancer agents
Britton, Robert G.,Horner-Glister, Emma,Pomenya, Odette A.,Smith, Ewan E.,Denton, Roanne,Jenkins, Paul R.,Steward, William P.,Brown, Karen,Gescher, Andreas,Sale, Stewart
experimental part, p. 952 - 958 (2012/10/08)
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 inhibi
