Discovery of 5??(2??(Phenylamino) pyrimidin??4??yl) thiazol??2 (3H)??one Derivatives as Potent Mnk2 Inhibitors: Synthesis, SAR Analysis and Biological Evaluation

S Diab, T Teo, M Kumarasiri, P Li, M Yu, F Lam…

文献索引：Diab, Sarah; Teo, Theodosia; Kumarasiri, Malika; Li, Peng; Yu, Mingfeng; Lam, Frankie; Basnet, Sunita K. C.; Sykes, Matthew J.; Albrecht, Hugo; Milne, Robert; Wang, Shudong ChemMedChem, 2014 , vol. 9, # 5 p. 962 - 972

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被引用次数: 20

摘要

Abstract Phosphorylation of eIF4E by human mitogen-activated protein kinase (MAPK)- interacting kinases (Mnks) is crucial for human tumourigenesis and development. Targeting Mnks may provide a novel anticancer therapeutic strategy. However, the lack of selective Mnk inhibitors has so far hampered pharmacological target validation and clinical drug development. Herein, we report, for the first time, the discovery of a series of 5-(2-( ...