期刊
MEDCHEMCOMM
卷 5, 期 1, 页码 41-46出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md00221g
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资金
- Health Research Council of New Zealand
- Maurice Wilkins Centre for Molecular Biodiscovery
- Pathway Therapeutics
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 p110 alpha-selective for compound 58 or p110 delta-selective for compound 57. The latter two compounds varied only in their sulphur oxidation state.
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