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Issue 11, 2012
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Small molecules targeting phosphoinositide 3-kinases

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Abstract

The phosphoinositide 3-kinase (PI3K) pathway is one of the most important signaling cascades in cancer, and PI3K is a well established target for anticancer therapy. Since the discovery of the first two compounds that inhibit PI3K, wortmannin and LY294002, a wealth of PI3K inhibitors of various chemotypes have been identified, and nearly twenty of them are currently in various stages of clinical trials. This review outlines the current landscape of the development of small molecule PI3K inhibitors with a focus on structure–activity relationships (SAR) and discussion of co-crystal structures.

Graphical abstract: Small molecules targeting phosphoinositide 3-kinases

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Article information


Submitted
14 Feb 2012
Accepted
05 May 2012
First published
11 May 2012

Med. Chem. Commun., 2012,3, 1337-1355
Article type
Review Article

Small molecules targeting phosphoinositide 3-kinases

P. Wu and Y. Hu, Med. Chem. Commun., 2012, 3, 1337
DOI: 10.1039/C2MD20044A

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