Carolin Schwehm
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
Authors
BARRIE KELLAM BARRIE.KELLAM@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry
Aimie Garces
STEPHEN HILL STEVE.HILL@NOTTINGHAM.AC.UK
Professor of Molecular Pharmacology
NICHOLAS KINDON Nicholas.Kindon@nottingham.ac.uk
Research Fellow
Dr TRACEY BRADSHAW tracey.bradshaw@nottingham.ac.uk
Associate Professor
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.
Citation
Schwehm, C., Kellam, B., Garces, A., Hill, S. J., Kindon, N., Bradshaw, T. D., …Stocks, M. (2017). 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. Journal of Medicinal Chemistry, 60(4), https://doi.org/10.1021/acs.jmedchem.6b01801
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 |
Files
acs.jmedchem.6b01801.pdf
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Copyright Statement
Copyright information regarding this work can be found at the following address: http://creativecommons.org/licenses/by-nc/4.0
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