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High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.
Wang J, Gong GQ, Zhou Y, Lee WJ, Buchanan CM, Denny WA, Rewcastle GW, Kendall JD, Dickson JMJ, Flanagan JU, Shepherd PR, Yang DH, Wang MW. Wang J, et al. Among authors: buchanan cm. Acta Pharmacol Sin. 2018 Nov;39(11):1816-1822. doi: 10.1038/s41401-018-0057-z. Epub 2018 Jul 10. Acta Pharmacol Sin. 2018. PMID: 29991713 Free PMC article.
Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.
Kendall JD, Giddens AC, Tsang KY, Frédérick R, Marshall ES, Singh R, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR. Kendall JD, et al. Bioorg Med Chem. 2012 Jan 1;20(1):58-68. doi: 10.1016/j.bmc.2011.11.031. Epub 2011 Nov 25. Bioorg Med Chem. 2012. PMID: 22177407
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.
Kendall JD, O'Connor PD, Marshall AJ, Frédérick R, Marshall ES, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR. Kendall JD, et al. Bioorg Med Chem. 2012 Jan 1;20(1):69-85. doi: 10.1016/j.bmc.2011.11.029. Epub 2011 Nov 25. Bioorg Med Chem. 2012. PMID: 22177405
Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
Rewcastle GW, Gamage SA, Flanagan JU, Frederick R, Denny WA, Baguley BC, Kestell P, Singh R, Kendall JD, Marshall ES, Lill CL, Lee WJ, Kolekar S, Buchanan CM, Jamieson SM, Shepherd PR. Rewcastle GW, et al. Among authors: buchanan cm. J Med Chem. 2011 Oct 27;54(20):7105-26. doi: 10.1021/jm200688y. Epub 2011 Sep 27. J Med Chem. 2011. PMID: 21882832
Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
Rewcastle GW, Gamage SA, Flanagan JU, Kendall JD, Denny WA, Baguley BC, Buchanan CM, Chao M, Kestell P, Kolekar S, Lee WJ, Lill CL, Malik A, Singh R, Jamieson SM, Shepherd PR. Rewcastle GW, et al. Among authors: buchanan cm. Eur J Med Chem. 2013 Jun;64:137-47. doi: 10.1016/j.ejmech.2013.03.038. Epub 2013 Apr 6. Eur J Med Chem. 2013. PMID: 23644197
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