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

Kendall, Jackie D.;Marshall, Andrew J.;Giddens, Anna C.;Tsang, Kit Yee;Shepherd, Peter R.;et.al.
(2014) MedChemComm — Vol. 5, n° 1, p. 41 [1-6] (2014)

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Authors
  • Kendall, Jackie D.
    Author
  • Marshall, Andrew J.
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  • Giddens, Anna C.
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  • Tsang, Kit Yee
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  • Frédérick, Raphaëlorcid-logoUCLouvain
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  • Shepherd, Peter R.
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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 p110a-selective for compound 58 or p110d-selective for compound 57. The latter two compounds varied only in their sulphur oxidation state.
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Kendall, J. D., Marshall, A. J., Giddens, A. C., Tsang, K. Y., Boyd, M., Frédérick, R., Lill, C. L., Lee, W.-J., Kolekar, S., Chao, M., Malik, A., Yu, S., Chaussade, C., Buchanan, C. M., Rewcastle, G. W., Baguley, B. C., Flanagan, J. U., Denny, W. A., & Shepherd, P. R. (2014). Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group. MedChemComm, 5(1), 41 [1-6]. https://doi.org/10.1039/C3MD00221G (Original work published 2014)