A Brief Overview of Two Major Strategies in Diversity-Oriented Synthesis: Build/Couple/Pair and Ring-Distortion

In the interdisciplinary research field of chemical biology and drug discovery, diversity-oriented synthesis (DOS) has become indispensable in the construction of novel small-molecule libraries rich in skeletal and stereochemical diversity. DOS aims to populate the unexplored chemical space with new...

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Bibliographic Details
Published in:Frontiers in chemistry 2018-10, Vol.6, p.507-507
Main Authors: Yi, Sihyeong, Varun, Begur Vasanthkumar, Choi, Yoona, Park, Seung Bum
Format: Article
Language:English
Subjects:
build/couple/pair
Chemistry
diversity-oriented synthesis
macrocycle
natural product
privileged structure
ring-distortion
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Summary:In the interdisciplinary research field of chemical biology and drug discovery, diversity-oriented synthesis (DOS) has become indispensable in the construction of novel small-molecule libraries rich in skeletal and stereochemical diversity. DOS aims to populate the unexplored chemical space with new potential bioactive molecules via forward synthetic analysis. Since the introduction of this concept by Schreiber, DOS has evolved along with many significant breakthroughs. It is therefore important to understand the key DOS strategies to build molecular diversity with maximized biological relevancy. Due to the length limitations of this mini review, we briefly discuss the recent DOS plans using build/couple/pair (B/C/P) and ring-distortion strategies for the synthesis of major biologically relevant target molecules like natural products and their related compounds, macrocycles, and privileged structures.
ISSN:2296-2646
2296-2646
DOI:10.3389/fchem.2018.00507