Browse views: by Year, by Function, by GLF, by Subfunction, by Conference, by Journal

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

Bruce, Ian, Akhlaq, Mohammed, Bloomfield, Graham, Budd, Emma, Cox, Brian, Finan, Peter, Gedeck, Peter, Hayler, Judy, Head, Denise, Kirman, Louise, Leblanc, Catherine, Le Grand, Darren, Owen, Charles, Oza, Mrinalini, Sviridenko, Lilya, Whitehead, Lewis, Keller, Thomas, McCarthy, Clive, O'Connor, Desmond, Pilgrim, Gaynor, 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.
Related URLs:
Date Deposited: 13 Oct 2015 13:14
Last Modified: 13 Oct 2015 13:14
URI: https://oak.novartis.com/id/eprint/7068

Search