Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors

…, R Katoch-Rouse, AS Kiselyov, D Sherman…

文献索引：Piatnitski Chekler, Eugene L.; Katoch-Rouse, Reeti; Kiselyov, Alexander S.; Sherman, Dan; Ouyang, Xiaohu; Kim, Ki; Wang, Ying; Hadari, Yaron R.; Doody, Jacqueline F. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4344 - 4347

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被引用次数: 11

摘要

We have discovered novel inhibitors of VEGFR-2 kinase with low nanomolar potency in both enzymatic and cell-based assays. Active series are heteroaryl-ketone compounds containing a central aromatic ring with either an indazolyl or indolyl keto group in the ortho orientation to the benzylic amine group (Fig. 1). The best compounds were demonstrated to be inactive against a small select panel of tyrosine and serine/threonine kinases with the ...