基于非肟吡唑的 B-Raf 激酶抑制剂。
Non-oxime pyrazole based inhibitors of B-Raf kinase.
机构信息
Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, United States.
出版信息
Bioorg Med Chem Lett. 2011 Jun 1;21(11):3488-92. doi: 10.1016/j.bmcl.2010.12.038. Epub 2010 Dec 17.
PMID:21536432
Abstract
The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyrazole 2a led to compound 38, a selective and potent B-Raf inhibitor.
摘要
报告了基于非肟吡唑的 B-Raf 抑制剂的合成和生物评价。已经制备了几种肟替代品，它们表现出优异的酶活性。进一步优化稠合吡唑 2a 得到化合物 38，它是一种选择性和有效的 B-Raf 抑制剂。
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