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:	http://www.ncbi.nlm.nih.gov/pubmed?term=...
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:	http://www.ncbi.nlm.nih.gov/pubmed?term=...
Date Deposited:	13 Oct 2015 13:14
Last Modified:	13 Oct 2015 13:14
URI:	https://oak.novartis.com/id/eprint/7068