2,4-二氨基嘧啶的甲磺酰胺环己基胺衍生物作为有效的 ALK 抑制剂。
Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.
机构信息
Worldwide Discovery Research, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA.
出版信息
Bioorg Med Chem Lett. 2011 Jul 1;21(13):3877-80. doi: 10.1016/j.bmcl.2011.05.040. Epub 2011 May 18.
PMID:21632243
Abstract
The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was achieved by conversion of the 2-amino group into a methanesulfonamide. Tumor growth inhibition was observed when an orally bioavailable analog was evaluated in a Karpas-299 tumor xenograft mouse model.
摘要
在一系列 2,4-二氨基嘧啶中，将 R,R-1,2-二氨基环己烷引入 C4 位，得到了一系列 ALK 抑制剂，其中通过将 2-氨基转化为甲磺酰胺，优化了活性。当在 Karpas-299 肿瘤异种移植小鼠模型中评估一种口服生物利用的类似物时，观察到肿瘤生长抑制。
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