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Anthranilic acid derivatives as multidrug resistance modulators

机译:邻氨基苯甲酸衍生物作为多药耐药性调节剂

摘要

Anthranilic acids of formula (I):wherein each of R to R9 is an organic substituent, n is 0 or 1, m is 0 or an integer of 1 to 6, q is 0 or 1, X is a direct bond, O, S, -S-(CH2)p or -O-(CHO2)p- wherein p is from 1 to 6 and Ar is an unsaturated carbocyclic or heterocyclic group, and the pharmaceutically acceptable salts thereof, have activity as inhibitors of P-glycoprotein and may thus be used, inter alia, as modulators of multidrug resistance in the treatment of multidrug resistant cancers, for example to potentiate the cytotoxicity of a cancer drug.
机译:式(I)的邻氨基苯甲酸:其中R至R9各自为有机取代基,n为0或1,m为0或1至6的整数,q为0或1,X为直接键,O, S,-S-(CH 2)p或-O-(CHO 2)p-,其中p为1至6,并且Ar为不饱和碳环或杂环基团,及其药学上可接受的盐具有作为P-糖蛋白抑制剂的活性。因此,其可以尤其在多药耐药性癌症的治疗中用作多药耐药性的调节剂,例如增强癌症药物的细胞毒性。

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