In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity at CYP-450

P Labrie, SP Maddaford, J Lacroix, C Catalano…

文献索引：Labrie, Philippe; Maddaford, Shawn. P.; Lacroix, Jacques; Catalano, Concettina; Lee, David K.H.; Rakhit, Suman; Gaudreault, Rene C. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 23 p. 7972 - 7987

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被引用次数: 20

摘要

Synthesis and in vitro cytotoxicity assays of new anthranilamide MDR modulators have been performed to assess their inhibition potency of the P-glycoprotein (P-gp) transporter. The aromatic spacer group between nitrogen atoms (N1 and N2) in the known inhibitor XR9576 was replaced with a flexible alkyl chain of 2 to 6 carbon atoms in length. 6, 7-Dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline and their open-chain N-methylhomoveratrylamine ...