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  • Natural products as lead structures: chemical transformations to create lead-like libraries

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    Author(s)
    Pascolutti, Mauro
    Quinn, Ronald J
    Griffith University Author(s)
    Quinn, Ronald J.
    Pascolutti, Mauro
    Year published
    2014
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    Abstract
    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.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.
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    Journal Title
    Drug Discovery Today
    Volume
    19
    Issue
    3
    DOI
    https://doi.org/10.1016/j.drudis.2013.10.013
    Copyright Statement
    © 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.
    Subject
    Medicinal and biomolecular chemistry not elsewhere classified
    Biochemistry and cell biology
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/66610
    Collection
    • Journal articles

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