2012
DOI: 10.1016/j.bmcl.2012.01.092
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Synthesis and structure–activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors

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Cited by 40 publications
(36 citation statements)
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“…16,17 However, the compounds were not suitable for in vivo studies due to high clearance in rat and mouse. Both 1 and 2 contain an embedded benzylamine moiety, a potential site for metabolism, which might contribute to the high clearance.…”
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confidence: 99%
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“…16,17 However, the compounds were not suitable for in vivo studies due to high clearance in rat and mouse. Both 1 and 2 contain an embedded benzylamine moiety, a potential site for metabolism, which might contribute to the high clearance.…”
mentioning
confidence: 99%
“…We were gratified to see that despite these potentially significant structural differences, both pyrazolopyrimidines retained the high PI3Kβ potency and excellent isoform selectivity observed with the other inhibitor series, as shown in Table 1. Because the SAR at this benzyl position had previously been well-established, 16 we were able to focus our further efforts mainly on the 2-methyl-3-trifluoromethyl benzyl analogues while we sought to better define the much less wellestablished hinge-binding and back-pocket SAR.…”
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confidence: 99%
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