Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors.

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ID: 58819
2019
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Abstract
The present work describes the syntheses of diverse triazole bridged flavonoid dimers and identifies potent, nontoxic, and highly selective BCRP inhibitors. A homodimer, , with -methoxycarbonylbenzyloxy substitution at C-3 of the flavone moieties and a triazole-containing linker (21 atoms between the two flavones) showed low toxicity (IC toward L929, 3T3, and HFF-1 > 100 μM), potent BCRP-inhibitory activity (EC = 1-2 nM), and high BCRP selectivity (BCRP selectivity over MRP1 and P-gp > 455-909). inhibits BCRP-ATPase activity, blocks the drug efflux activity of BCRP, elevates the intracellular drug accumulation, and finally restores the drug sensitivity of BCRP-overexpressing cells. It does not down-regulate the surface BCRP protein expression to enhance the drug retention. Therefore, and similar flavonoid dimers appear to be promising candidates for further development into combination therapy to overcome MDR cancers with BCRP overexpression.
Reference Key
zhu2019triazolejournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Zhu, Xuezhen;Wong, Iris L K;Chan, Kin-Fai;Cui, Jiahua;Law, Man Chun;Chong, Tsz Cheung;Hu, Xuesen;Chow, Larry M C;Chan, Tak Hang;
Journal Journal of medicinal chemistry
Year 2019
DOI
10.1021/acs.jmedchem.9b00963
URL
Keywords
2 1 Docking Triazole DFT qsar 3]triazolo[4 5-d]pyrimidine analogues pyrimidine

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