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Molecules 2014, 19(11), 17221-17255; doi:10.3390/molecules191117221

Diversity-Oriented Synthetic Strategies Applied to Cancer Chemical Biology and Drug Discovery

1
Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK
2
Division of Chemistry and Environmental Science, School of Science and the Environment, Faculty of Science and Engineering, Manchester Metropolitan University, John Dalton Building, Chester Street, Manchester M1 5GD, UK
*
Authors to whom correspondence should be addressed.
Received: 22 August 2014 / Revised: 13 October 2014 / Accepted: 17 October 2014 / Published: 27 October 2014
(This article belongs to the Special Issue Recent Advances in Diversity-Oriented Synthesis)

Abstract

How can diversity-oriented strategies for chemical synthesis provide chemical tools to help shape our understanding of complex cancer pathways and progress anti-cancer drug discovery efforts? This review (surveying the literature from 2003 to the present) considers the applications of diversity-oriented synthesis (DOS), biology-oriented synthesis (BIOS) and associated strategies to cancer biology and drug discovery, summarising the syntheses of novel and often highly complex scaffolds from pluripotent or synthetically versatile building blocks. We highlight the role of diversity-oriented synthetic strategies in producing new chemical tools to interrogate cancer biology pathways through the assembly of relevant libraries and their application to phenotypic and biochemical screens. The use of diversity-oriented strategies to explore structure-activity relationships in more advanced drug discovery projects is discussed. We show how considering appropriate and variable focus in library design has provided a spectrum of DOS approaches relevant at all stages in anti-cancer drug discovery. View Full-Text
Keywords: diversity-oriented synthesis (DOS); biology-oriented synthesis (BIOS); cancer; chemical tools; drug discovery diversity-oriented synthesis (DOS); biology-oriented synthesis (BIOS); cancer; chemical tools; drug discovery
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Collins, I.; Jones, A.M. Diversity-Oriented Synthetic Strategies Applied to Cancer Chemical Biology and Drug Discovery. Molecules 2014, 19, 17221-17255.

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