Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1, 2, 4] triazolo [1, 5-a] pyridine derivatives with slow dissociation kinetics

…, N Miyamoto, M Tawada, H Iwata, H Miki, A Hori…

文献索引：Oguro, Yuya; Cary, Douglas R.; Miyamoto, Naoki; Tawada, Michiko; Iwata, Hidehisa; Miki, Hiroshi; Hori, Akira; Imamura, Shinichi Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 15 p. 4714 - 4729

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被引用次数: 12

摘要

For the purpose of discovering novel type-II inhibitors of vascular endothelial growth factor receptor 2 (VEGFR2) kinase, we designed and synthesized 5, 6-fused heterocyclic compounds bearing a anilide group. A co-crystal structure analysis of imidazo [1, 2-b] pyridazine derivative 2 with VEGFR2 revealed that the N1-nitrogen of imidazo [1, 2-b] pyridazine core interacts with the backbone NH group of Cys919. To retain this essential ...