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

Drug Discov Today. 2014 Mar;19(3):215-21. doi: 10.1016/j.drudis.2013.10.013. Epub 2013 Oct 27.

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.

Publication types

  • Review

MeSH terms

  • Biological Products / chemistry*
  • Chemistry, Pharmaceutical
  • Drug Design*
  • Humans
  • Molecular Weight
  • Small Molecule Libraries / chemistry

Substances

  • Biological Products
  • Small Molecule Libraries