Skip to main content

Research Repository

Advanced Search

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) inhib

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

Carolin Schwehm paxcs4@exmail.nottingham.ac.uk

Barrie Kellam barrie.kellam@nottingham.ac.uk

Stephen J. Hill

Nicholas Kindon

Tracey D. Bradshaw

Jin Li Jin.Li@Hitgen.com

Simon J.F. Macdonald simon.jf.macdonald@gsk.com

James E. Rowedder

Leigh A. Stoddart

Michael Stocks michael.stocks@nottingham.ac.uk



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 δ 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
Publication Date Jan 27, 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
APA6 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
DOI https://doi.org/10.1021/acs.jmedchem.6b01801
Publisher URL http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b01801
Copyright Statement Copyright information regarding this work can be found at the following address: http://creativecommons.org/licenses/by-nc/4.0

Files

acs.jmedchem.6b01801.pdf (6.3 Mb)
PDF

Copyright Statement
Copyright information regarding this work can be found at the following address: http://creativecommons.org/licenses/by-nc/4.0





You might also like



Downloadable Citations

;