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Lead‐Oriented Synthesis: A New Opportunity for Synthetic Chemistry
Author(s) -
Nadin Alan,
Hattotuwagama Channa,
Churcher Ian
Publication year - 2012
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.201105840
Subject(s) - lead (geology) , drug discovery , pharmaceutical industry , nanotechnology , chemistry , drug development , combinatorial chemistry , biochemical engineering , drug , data science , computer science , engineering , pharmacology , materials science , medicine , biology , paleontology , biochemistry
The pharmaceutical industry remains solely reliant on synthetic chemistry methodology to prepare compounds for small‐molecule drug discovery programmes. The importance of the physicochemical properties of these molecules in determining their success in drug development is now well understood but we present here data suggesting that much synthetic methodology is unintentionally predisposed to producing molecules with poorer drug‐like properties. This bias may have ramifications to the early hit‐ and lead‐finding phases of the drug discovery process when larger numbers of compounds from array techniques are prepared. To address this issue we describe for the first time the concept of lead‐oriented synthesis and the opportunity for its adoption to increase the range and quality of molecules used to develop new medicines.