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Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors

Schwehm, Carolin; Kellam, Barrie; Garces, Aimie; Hill, Stephen J.; Kindon, Nicholas; Bradshaw, Tracey D.; Li, Jin; Macdonald, Simon J.F.; Rowedder, James E.; Stoddart, Leigh A.; Stocks, Michael

Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors Thumbnail


Authors

Carolin Schwehm

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BARRIE KELLAM BARRIE.KELLAM@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry

Aimie Garces

STEPHEN HILL STEVE.HILL@NOTTINGHAM.AC.UK
Professor of Molecular Pharmacology

Jin Li

Simon J.F. Macdonald

James E. Rowedder

Leigh A. Stoddart

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



Abstract

A novel molecular scaffold has been synthesized, and its incorporation into new analogues of biologically active molecules across multiple target classes will be discussed. In these studies, we have shown use of the tricyclic scaffold to synthesize potent inhibitors of the serine peptidase DPP-4, antagonists of the CCR5 receptor, and highly potent and selective PI3K ? isoform inhibitors. We also describe the predicted physicochemical properties of the resulting inhibitors and conclude that the tractable molecular scaffold could have potential application in future drug discovery programs.

Journal Article Type Article
Acceptance Date Jan 26, 2017
Publication Date Jan 27, 2017
Deposit Date Jul 11, 2017
Publicly Available Date Jul 11, 2017
Journal Journal of Medicinal Chemistry
Print ISSN 0022-2623
Electronic ISSN 1520-4804
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 60
Issue 4
DOI https://doi.org/10.1021/acs.jmedchem.6b01801
Public URL https://nottingham-repository.worktribe.com/output/838861
Publisher URL http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b01801

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