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Development of isoform selective PI 3-Kinase inhibitors as pharmacological tools for elucidating the PI3K pathway

Bruce, Ian and Akhlaq, Mohammed and Bloomfield, Graham and Budd, Emma and Cox, Brian and Finan, Peter and Gedeck, Peter and Hayler, Judy and Head, Denise and Kirman, Louise and Leblanc, Catherine and Le Grand, Darren and Owen, Charles and Oza, Mrinalini and Sviridenko, Lilya and Whitehead, Lewis and Keller, Thomas and McCarthy, Clive and O'Connor, Desmond and Pilgrim, Gaynor and Press, Nicola and Cuenoud, Bernard (2012) Development of isoform selective PI 3-Kinase inhibitors as pharmacological tools for elucidating the PI3K pathway. Bioorganic & Medicinal Chemistry Letters, 22 (17). pp. 5445-5450. ISSN 0960-894X

Abstract

Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had good cellular activity and were selective against protein kinases and other members of the PI3K superfamily including mTOR and DNA-PK.

Item Type: Article
Related URLs:
Additional Information: Revised Manuscript. QAL964 removed to be published seperately in due course. A paid open access option is available for this journal.
Keywords: PI 3-Kinase inhibitors, pharmacological tools, Aminothiazoles, isoform selectivity.
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Date Deposited: 13 Oct 2015 13:14
Last Modified: 13 Oct 2015 13:14
URI: https://oak.novartis.com/id/eprint/7068

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