Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker groupElectronic supplementary information (ESI) available. See DOI: 10.1039/c3md00221g
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 BR...
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| creator | Kendall, Jackie D Marshall, Andrew J Giddens, Anna C Tsang, Kit Yee Boyd, Maruta Frédérick, Raphaël Lill, Claire L Lee, Woo-Jeong Kolekar, Sharada Chao, Mindy Malik, Alisha Yu, Shuqiao Chaussade, Claire Buchanan, Christina M Rewcastle, Gordon W Baguley, Bruce C Flanagan, Jack U Denny, William A Shepherd, Peter R |
| description | 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.
SAR of novel PI3K inhibitors is described. |
| doi_str_mv | 10.1039/c3md00221g |
| format | Article |
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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.
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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.
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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.
SAR of novel PI3K inhibitors is described.</abstract><doi>10.1039/c3md00221g</doi><tpages>6</tpages></addata></record> |
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| source | Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection |
| title | Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker groupElectronic supplementary information (ESI) available. See DOI: 10.1039/c3md00221g |
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