Abstract
Small bioactive molecules are pre-requisite for any discovery discipline. Being aware of the fact that bioactivity is not randomly dispersed in the vast chemical space, chemists have been developing hypothesis that can provide access to these islands of bioactivities. Natural products have always been a source of inspiration and their structural motifs provide biologically relevant starting points for library synthesis. In addition to that, Diversity Oriented Synthesis (DOS) and Biology Oriented Synthesis (BIOS) have emerged other tools to guide synthesis design and help enrich compound collections in biological activities. Coherent developments in chem- and bioinformatic tools and in organic synthesis methods targeting efficient synthesis of compound collections are required to identify interesting molecules that can be employed as probes in chemical biology research and as drug candidates in medicinal chemistry investigations.
Keywords: Natural products, diversity oriented synthesis, biology oriented synthesis, compound libraries, small molecules, drug discovery, bioactivity, protein inhibitor, cyclopeptides, chemical space
Current Drug Targets
Title: Exploring and Exploiting Biologically Relevant Chemical Space
Volume: 12 Issue: 11
Author(s): Luc Eberhardt, Kamal Kumar and Herbert Waldmann
Affiliation:
Keywords: Natural products, diversity oriented synthesis, biology oriented synthesis, compound libraries, small molecules, drug discovery, bioactivity, protein inhibitor, cyclopeptides, chemical space
Abstract: Small bioactive molecules are pre-requisite for any discovery discipline. Being aware of the fact that bioactivity is not randomly dispersed in the vast chemical space, chemists have been developing hypothesis that can provide access to these islands of bioactivities. Natural products have always been a source of inspiration and their structural motifs provide biologically relevant starting points for library synthesis. In addition to that, Diversity Oriented Synthesis (DOS) and Biology Oriented Synthesis (BIOS) have emerged other tools to guide synthesis design and help enrich compound collections in biological activities. Coherent developments in chem- and bioinformatic tools and in organic synthesis methods targeting efficient synthesis of compound collections are required to identify interesting molecules that can be employed as probes in chemical biology research and as drug candidates in medicinal chemistry investigations.
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Cite this article as:
Eberhardt Luc, Kumar Kamal and Waldmann Herbert, Exploring and Exploiting Biologically Relevant Chemical Space, Current Drug Targets 2011; 12 (11) . https://dx.doi.org/10.2174/138945011798109482
DOI https://dx.doi.org/10.2174/138945011798109482 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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