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Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway |
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| Authors: | Ian Bruce Mohammed Akhlaq Graham C Bloomfield Emma Budd Brian Cox Bernard Cuenoud Peter Finan Peter Gedeck Julia Hatto Judy F Hayler Denise Head Thomas Keller Louise Kirman Catherine Leblanc Darren Le Grand Clive McCarthy Desmond O'Connor Charles Owen Mrinalini S Oza Gaynor Pilgrim Nicola E Press Lilya Sviridenko Lewis Whitehead |
| Institution: | Novartis Institutes for Biomedical Research, Respiratory Disease Area, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK. |
| 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. |
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