Bioorganic & medicinal chemistry letters

Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly

T Irie, I Fujii, M Sawa

文献索引：Irie, Takayuki; Fujii, Ikuo; Sawa, Masaaki Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 591 - 596

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被引用次数: 12

摘要

Fragment-based lead discovery is a new approach for lead generation that has emerged in the past decade. Because the initial fragments identified in the fragment screening typically show weak binding affinity, an intensive medicinal chemistry effort would be required to grow initial fragments into a potential lead compound. Here we demonstrate a kinase focused evolved fragment (KFEF) library, constructed by click chemistry-based fragment ...