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Page 1
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: san miguel t. J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25. J Med Chem. 2016. PMID: 27411843
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
D'Angelo ND, Kim TS, Andrews K, Booker SK, Caenepeel S, Chen K, D'Amico D, Freeman D, Jiang J, Liu L, McCarter JD, San Miguel T, Mullady EL, Schrag M, Subramanian R, Tang J, Wahl RC, Wang L, Whittington DA, Wu T, Xi N, Xu Y, Yakowec P, Yang K, Zalameda LP, Zhang N, Hughes P, Norman MH. D'Angelo ND, et al. Among authors: san miguel t. J Med Chem. 2011 Mar 24;54(6):1789-811. doi: 10.1021/jm1014605. Epub 2011 Feb 18. J Med Chem. 2011. PMID: 21332118
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Nishimura N, Siegmund A, Liu L, Yang K, Bryan MC, Andrews KL, Bo Y, Booker SK, Caenepeel S, Freeman D, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Whittington DA, Zalameda L, Zhang N, Hughes PE, Norman MH. Nishimura N, et al. Among authors: san miguel t. J Med Chem. 2011 Jul 14;54(13):4735-51. doi: 10.1021/jm200386s. Epub 2011 Jun 20. J Med Chem. 2011. PMID: 21612232
Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.
Stec MM, Andrews KL, Booker SK, Caenepeel S, Freeman DJ, Jiang J, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Yang K, Zalameda LP, Zhang N, Hughes PE, Norman MH. Stec MM, et al. Among authors: san miguel t. J Med Chem. 2011 Jul 28;54(14):5174-84. doi: 10.1021/jm2004442. Epub 2011 Jun 29. J Med Chem. 2011. PMID: 21714526
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.
Lanman BA, Reed AB, Cee VJ, Hong FT, Pettus LH, Wurz RP, Andrews KL, Jiang J, McCarter JD, Mullady EL, San Miguel T, Subramanian R, Wang L, Whittington DA, Wu T, Zalameda L, Zhang N, Tasker AS, Hughes PE, Norman MH. Lanman BA, et al. Among authors: san miguel t. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5630-5634. doi: 10.1016/j.bmcl.2014.10.085. Epub 2014 Nov 1. Bioorg Med Chem Lett. 2014. PMID: 25466188
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. Among authors: san miguel t. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
Synthesis and SAR study of potent and selective PI3Kδ inhibitors.
Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD. Bui M, et al. Among authors: san miguel t. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17. Bioorg Med Chem Lett. 2015. PMID: 25666823
The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.
Stec MM, Andrews KL, Bo Y, Caenepeel S, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Whittington DA, Wang L, Wu T, Zalameda LP, Zhang N, Hughes PE, Norman MH. Stec MM, et al. Among authors: san miguel t. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4136-42. doi: 10.1016/j.bmcl.2015.08.016. Epub 2015 Aug 8. Bioorg Med Chem Lett. 2015. PMID: 26298499
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Shin Y, Suchomel J, Cardozo M, Duquette J, He X, Henne K, Hu YL, Kelly RC, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wong S, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Shin Y, et al. Among authors: san miguel t. J Med Chem. 2016 Jan 14;59(1):431-47. doi: 10.1021/acs.jmedchem.5b01651. Epub 2015 Dec 21. J Med Chem. 2016. PMID: 26652588
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: san miguel t. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
54 results