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Scaffold Diversity Synthesis and Its Application in Probe and Drug Discovery
Author(s) -
GarciaCastro Miguel,
Zimmermann Stefan,
Sankar Muthukumar G.,
Kumar Kamal
Publication year - 2016
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201508818
Subject(s) - scaffold , drug discovery , computer science , diversity (politics) , nanotechnology , data science , biochemical engineering , combinatorial chemistry , engineering , biology , chemistry , bioinformatics , materials science , database , sociology , anthropology
Scaffold diversity is a crucial feature of compound collections that has a huge impact on their success in biological screenings. The synthesis of highly complex and diverse scaffolds, which could be based on natural products, for example, is an arduous task that requires expertise in various aspects of organic synthesis and structural analysis. This challenge has been addressed by a number of synthesis designs, which employ natural products as a source of scaffold diversity, transform suitably designed common intermediates into various molecular frameworks, or entail highly concise synthetic routes to a number of distinct and complex scaffolds. In this Minireview, we highlight recent synthetic developments towards the construction of diverse and complex scaffolds and the application of the resulting compound collections in drug and probe discovery.