Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway

Bruce, Ian, Akhlaq, Mohammed, Bloomfield, Graham C, Budd, Emma, Cox, Brian, Cuenoud, Bernard, Finan, Peter, Gedeck, Peter, Hatto, Julia, Hayler, Judy F, Head, Denise, Keller, Thomas, Kirman, Louise, Leblanc, Catherine, Le Grand, Darren, McCarthy, Clive, O'Connor, Desmond, Owen, Charles, Oza, Mrinalini S, Pilgrim, Gaynor, Press, Nicola E, Sviridenko, Lilya and Whitehead, Lewis (2012) Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway. Bioorganic and Medicinal Chemistry Letters, 22 (17). pp. 5445-5450. ISSN 0960-894X

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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
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 12 Jan 2015 12:10
Last Modified: 01 Jun 2015 15:34
URI: http://sro.sussex.ac.uk/id/eprint/52042
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