发现4-氮杂吲哚作为c-Met激酶的新型抑制剂。
Discovery of 4-azaindoles as novel inhibitors of c-Met kinase.
作者信息
Porter John, Lumb Simon, Franklin Richard J, Gascon-Simorte Jose M, Calmiano Mark, Riche Kelly Le, Lallemand Bénédicte, Keyaerts Jean, Edwards Helen, Maloney Alison, Delgado Jean, King Lloyd, Foley Anne, Lecomte Fabien, Reuberson James, Meier Christoph, Batchelor Mark
机构信息
UCB Celltech, Slough, United Kingdom.
出版信息
Bioorg Med Chem Lett. 2009 May 15;19(10):2780-4. doi: 10.1016/j.bmcl.2009.03.110. Epub 2009 Mar 27.
PMID:19369077
Abstract
A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.
摘要
描述了一系列c-Met激酶的4-氮杂吲哚抑制剂。通过X射线晶体结构证实了假定的结合模式，并基于该结构进行了系列优化。讨论了该系列开发的未来方向。
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