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ID: ALA1143794

Journal: Bioorg Med Chem Lett

Title: Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.

Authors: Noronha G, Barrett K, Boccia A, Brodhag T, Cao J, Chow CP, Dneprovskaia E, Doukas J, Fine R, Gong X, Gritzen C, Gu H, Hanna E, Hood JD, Hu S, Kang X, Key J, Klebansky B, Kousba A, Li G, Lohse D, Mak CC, McPherson A, Palanki MS, Pathak VP, Renick J, Shi F, Soll R, Splittgerber U, Stoughton S, Tang S, Yee S, Zeng B, Zhao N, Zhu H.

Abstract: We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines and in animal models of tumor growth.

CiteXplore: 17113292

DOI: 10.1016/j.bmcl.2006.11.006