Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction.

Cynthia Palmer,Mason Pairish,Susan Kephart,Djamal Bouzida,Jingrong Cui,Judith Deal,Liming Dong,Danlin Gu,Angelica Linton,Indrawan McAlpine,Shinji Yamazaki,Evan Smith,Annette John-Baptiste,Shubha Bagrodia,Robert Kania,Chuangxing Guo

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

Potent bRAF inhibitors containing 3-methoxy-2-aminopyridine moiety were shown to be representative examples of an electron rich heteroaryl associated with time-dependent drug–drug interactions and mutagenicity. These risks may be reduced by either reducing electron density or preventing the formation of the mutagenic metabolite.

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关键词

Bioactivation,AMES positive,TDI,Toxicity,Electron rich heteroaryls,Kinase inhibitor,Reactive metabolite,Mutagenicity,Time dependent drug–drug interaction

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