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Issue 1, 2014
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Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group

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Abstract

As part of our investigation into the pyrazolo[1,5-a]pyridines as novel PI3K inhibitors, we report a range of analogues where the central linker portion of the molecule was varied while retaining the pyrazolo[1,5-a]pyridine and arylsulfonyl or arylcarbonyl groups. Isostere generating software BROOD was used to assist with producing ideas. The isoform selectivity of the compounds varied from pan-PI3K for compound 41 to p110α-selective for compound 58 or p110δ-selective for compound 57. The latter two compounds varied only in their sulphur oxidation state.

Graphical abstract: Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group

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Publication details

The article was received on 30 Jul 2013, accepted on 26 Oct 2013 and first published on 30 Oct 2013


Article type: Concise Article
DOI: 10.1039/C3MD00221G
Citation: Med. Chem. Commun., 2014,5, 41-46
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    Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group

    J. D. Kendall, A. J. Marshall, A. C. Giddens, K. Y. Tsang, M. Boyd, R. Frédérick, C. L. Lill, W. Lee, S. Kolekar, M. Chao, A. Malik, S. Yu, C. Chaussade, C. M. Buchanan, G. W. Rewcastle, B. C. Baguley, J. U. Flanagan, W. A. Denny and P. R. Shepherd, Med. Chem. Commun., 2014, 5, 41
    DOI: 10.1039/C3MD00221G

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