Disubstituted indazoles as potent antagonists of the integrin αvβ3

…, DP Modi, GA Cain, MH Corjay, SA Mousa…

文献索引：Batt, Douglas G.; Harlow, Patricia P.; Barbera, Frank A.; Spitz, Susan M.; Wexler, Ruth R.; Jadhav, Prabhakar K.; Petraitis, Joseph J.; Houghton, Gregory C.; Modi, Dilip P.; Cain, Gary A.; Corjay, Martha H.; Mousa, Shaker A.; Bouchard, Peter J.; Forsythe, Mark S. Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 41 - 58

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被引用次数: 96

摘要

A new series of indazole-containing αvβ3 integrin antagonists is described. Starting with lead compound 18a, variations in a number of structural features were explored with respect to inhibition of the binding of β3-transfected 293 cells to fibrinogen and to selectivity for αvβ3 over GPIIbIIIa, another RGD-binding integrin. Indazoles attached to a 2-aminopyridine or 2- aminoimidazole by a propylene linker at the indazole 1-position and to a ...