Natural products as lead structures: chemical transformations to create lead-like libraries
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In this review, we analyze and illustrate the variation of the two main lead-like descriptors [molecular weight (MW) and the partition coefficient (logP)] in the generation of libraries in which a natural product (NP) is used as the guiding structure. Despite the different approaches used to create NP-like libraries, controlling these descriptors during the synthetic process is important to generate lead-like libraries. From this analysis, we present a schematic approach to the generation of lead-like libraries that can be applied to any starting NP.
Drug Discovery Today
© 2014 The Authors. Published by Elsevier Inc. This is an open access article under the Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) (http://creativecommons.org/licenses/by/3.0/) that permits non-commercial distribution, and reproduction in any medium, provided the original work is properly cited.
Medicinal and Biomolecular Chemistry not elsewhere classified