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Class 1 PI3K clinical candidates and recent inhibitor design strategies: a medicinal chemistry perspective

Garces, Aimie E.; Stocks, Michael J.

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Authors

Aimie E. Garces

MICHAEL STOCKS MICHAEL.STOCKS@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry and Drug Discovery



Abstract

Phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylate the 3-OH of the inositol ring of phosphoinositides, and deregulation of this pathway has implications in many diseases. The search for novel PI3K inhibitors has been at the forefront of academic and industrial medicinal chemistry with over 600 medicinal chemistry-based publications and patents appearing to date, leading to 38 clinical candidates and the launch of two drugs, idelalisib in 2014 and copanlisib in 2017. This Perspective will discuss medicinal chemistry design approaches to novel isoform-selective inhibitors through consideration of brief case histories of compounds that have progressed into clinical development or that have revealed new structural motifs in this highly competitive area of research.

Journal Article Type Article
Acceptance Date Dec 24, 2018
Online Publication Date Dec 24, 2018
Publication Date May 23, 2019
Deposit Date Jan 3, 2019
Publicly Available Date Dec 25, 2019
Journal Journal of Medicinal Chemistry
Print ISSN 0022-2623
Electronic ISSN 1520-4804
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 62
Issue 10
Pages 4815-4850
DOI https://doi.org/10.1021/acs.jmedchem.8b01492
Keywords Molecular Medicine; Drug Discovery
Public URL https://nottingham-repository.worktribe.com/output/1441736
Publisher URL https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01492

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