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[(Alkylamino) methyl] acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase

P Traxler, U Trinks, E Buchdunger, H Mett…

文献索引:Traxler, Peter; Trinks, Uwe; Buchdunger, Elisabeth; Mett, Helmut; Meyer, Thomas; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 13 p. 2441 - 2448

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被引用次数: 90

摘要

[(Alkylamino) methyllacrylophenones and (alkylamino) propiophenones, bearing a spacer moiety such as the benzyloxy or (benzoylsulfony1) oxy group in the 4-position, represent a novel class of inhibitors of the epidermal growth factor (EGF) receptor protein tyrosine kinase with a high degree of selectivity versus other tyrosine and serineithreonine kinases. The- most active compounds inhibited the EGF receptor protein tyrosine kinase from A431 cell ...