Synthesis of Unprecedented Scaffold Diversity

摘要

The screening of compound libraries to identify useful modulators of biological systems is a fundamental process in chemical biology studies.However,a crucial consideration is what compounds to use.When such processes are unbiased,for example in the case of a phenotypic screen where the biological target is unknown,libraries which contain compounds displaying a broad range of biological activities are particularly valuable.As biological function is intrinsically dependent upon molecular structure,the design and synthesis of structurally diverse compound libraries has attracted considerable attention.In particular,variation in the molecular scaffolds present in the library(so-called scaffold diversity)is crucial,with small multiple-scaffold libraries generally regarded as superior to large single-scaffold libraries in terms of biorelevant diversity.