吡唑并[1,5-a]嘧啶-3-羧酸酯作为B-Raf激酶抑制剂的鉴定。
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.
作者信息
Gopalsamy Ariamala, Ciszewski Greg, Hu Yongbo, Lee Frederick, Feldberg Larry, Frommer Eileen, Kim Steven, Collins Karen, Wojciechowicz Donald, Mallon Robert
机构信息
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2009 May 15;19(10):2735-8. doi: 10.1016/j.bmcl.2009.03.129. Epub 2009 Mar 28.
B-Raf kinase plays a critical role in the Raf-MEK-ERK signaling pathway and inhibitors of B-Raf could be used in the treatment of melanomas, colorectal cancer, and other Ras related human cancers. We have identified novel small molecule pyrazolo[1,5-a]pyrimidine derivatives as B-Raf kinase inhibitors. Structure-activity relationship was generated for various regions of the scaffold to improve the biochemical profile.
B-Raf激酶在Raf-MEK-ERK信号通路中起关键作用，B-Raf抑制剂可用于治疗黑色素瘤、结直肠癌及其他与Ras相关的人类癌症。我们已鉴定出新型小分子吡唑并[1,5-a]嘧啶衍生物作为B-Raf激酶抑制剂。为改善生化特性，对该支架的各个区域建立了构效关系。
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