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
Copyright 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