《Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors》 was written by 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. Related Products of 1129-28-8This research focused ontriazole bridged flavonoid dimer breast cancer SAR docking. The article conveys some information:
The present work describes the syntheses of diverse triazole bridged flavonoid dimers and identifies potent, nontoxic, and highly selective BCRP inhibitors. A homodimer, Ac22(Az8)2, with m-methoxycarbonylbenzyloxy substitution at C-3 of the flavone moieties and a bis-triazole-containing linker (21 atoms between the two flavones) showed low toxicity (IC50 toward L929, 3T3, and HFF-1 > 100 μM), potent BCRP-inhibitory activity (EC50 = 1-2 nM), and high BCRP selectivity (BCRP selectivity over MRP1 and P-gp > 455-909). Ac22(Az8)2 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, Ac22(Az8)2 and similar flavonoid dimers appear to be promising candidates for further development into combination therapy to overcome MDR cancers with BCRP overexpression. In the experimental materials used by the author, we found Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Related Products of 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Related Products of 1129-28-8 In contrast, terrestrial plants account only for a few bromine-containing compounds.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary