Identification of new 4-N-substituted 6-aryl-7H-pyrrolo [2, 3-d] pyrimidine-4-amines as highly potent EGFR-TK inhibitors with Src-family activity

…, S Bugge, G Bjørkøy, E Sundby, BH Hoff

文献索引：Kaspersen, Svein Jacob; Han, Jin; Norsett, Kristin G.; Rydsa, Line; Kjobli, Eli; Bugge, Steffen; Bjorkoy, Geir; Sundby, Eirik; Hoff, Bard Helge European Journal of Pharmaceutical Sciences, 2014 , vol. 59, # 1 p. 69 - 82

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被引用次数: 5

摘要

Abstract The epidermal growth factor receptor is an important target in molecular cancer therapy. Herein, the enzymatic inhibition potential of a series of chiral and non chiral pyrrolopyrimidine based derivatives have been investigated and optimised. Overall, seven new compounds were identified having enzymatic IC 50 values comparable to or better than the commercial drug Erlotinib. High activity was also confirmed towards the epidermal ...