期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 1, 页码 115-125出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm2010767
关键词
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Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][1,2,4]triazine ALK inhibitors are described along with synthesis and biological activity. Piperidine-derived analogues showing minimal microsomal reactive metabolite formation were discovered. Potent, selective, and metabolically stable ALK inhibitors from this class were identified, and an orally bioavailable compound (32) with antitumor efficacy in ALK-driven xenografts in mouse models was extensively characterized.
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