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…

Index: 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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Citation Number: 20

Abstract

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-( ...