Flavonoid dimers and methods of making and using such

Details Flavonoid dimers and methods of making and using such Flavonoid dimers and methods of making and using such

C - Chemistry, Metallurgy

07

D

C07D 311/30 (2006.01) A61K 31/35 (2006.01) A61K 31/352 (2006.01) A61K 31/365 (2006.01) A61P 35/00 (2006.01) C07D 311/32 (2006.01)

Patent

CA 2652617

Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over- expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.

La résistance pléiotrope pose un problème important en chimiothérapie anticancéreuse. Le mécanisme de résistance le mieux caractérisé a comme médiateur la surexpression des transporteurs d'effluence des médicaments, la P-glycoprotéine (P-gp), qui pompent divers médicaments anticancéreux hors des cellules, ce qui aboutit à une diminution de l'accumulation intracellulaire des médicaments. L'invention propose ainsi une gamme de dimères de flavonoïdes liés entre eux par des groupes de liaison de diverses longueurs. Ces dimères de flavonoïdes s'avèrent des modulateurs efficaces de la P-gp qui accroissent la cytotoxicité des médicaments anticancéreux in vitro et renforce de façon considérable leur effet d'accumulation intracellulaire des médicaments. Il s'avère en outre que les dimères de flavonoïdes de l'invention conviennent également pour la réduction de la résistance aux médicaments pour le traitement des maladies parasitaires.

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