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Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
Sutherlin DP, Sampath D, Berry M, Castanedo G, Chang Z, Chuckowree I, Dotson J, Folkes A, Friedman L, Goldsmith R, Heffron T, Lee L, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Prior WW, Salphati L, Sideris S, Tian Q, Tsui V, Wan NC, Wang S, Wiesmann C, Wong S, Zhu BY. Sutherlin DP, et al. Among authors: mathieu s. J Med Chem. 2010 Feb 11;53(3):1086-97. doi: 10.1021/jm901284w. J Med Chem. 2010. PMID: 20050669
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Heffron TP, et al. Among authors: mathieu s. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20346656
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J, Heffron T, Lesnick J, Lewis C, Mathieu S, Murray J, Nonomiya J, Pang J, Pegg N, Prior WW, Rouge L, Salphati L, Sampath D, Tian Q, Tsui V, Wan NC, Wang S, Wei B, Wiesmann C, Wu P, Zhu BY, Olivero A. Sutherlin DP, et al. Among authors: mathieu s. J Med Chem. 2011 Nov 10;54(21):7579-87. doi: 10.1021/jm2009327. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21981714
Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.
Heffron TP, Wei B, Olivero A, Staben ST, Tsui V, Do S, Dotson J, Folkes AJ, Goldsmith P, Goldsmith R, Gunzner J, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Shuttleworth S, Sutherlin DP, Wan NC, Wang S, Wiesmann C, Zhu BY. Heffron TP, et al. Among authors: mathieu s. J Med Chem. 2011 Nov 24;54(22):7815-33. doi: 10.1021/jm2007084. Epub 2011 Oct 21. J Med Chem. 2011. PMID: 21985639
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J. Mathieu S, et al. J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29. J Med Chem. 2012. PMID: 22335519
The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.
Ren L, Ahrendt KA, Grina J, Laird ER, Buckmelter AJ, Hansen JD, Newhouse B, Moreno D, Wenglowsky S, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Risom T, Sturgis HL, Voegtli WC, Mathieu S. Ren L, et al. Among authors: mathieu s. Bioorg Med Chem Lett. 2012 May 15;22(10):3387-91. doi: 10.1016/j.bmcl.2012.04.015. Epub 2012 Apr 10. Bioorg Med Chem Lett. 2012. PMID: 22534450
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Wenglowsky S, Ren L, Grina J, Hansen JD, Laird ER, Moreno D, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Sturgis HL, Voegtli WC, Vigers G, Willis B, Mathieu S, Rudolph J. Wenglowsky S, et al. Among authors: mathieu s. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1923-7. doi: 10.1016/j.bmcl.2014.03.007. Epub 2014 Mar 13. Bioorg Med Chem Lett. 2014. PMID: 24675381
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
Wenglowsky S, Ren L, Ahrendt KA, Laird ER, Aliagas I, Alicke B, Buckmelter AJ, Choo EF, Dinkel V, Feng B, Gloor SL, Gould SE, Gross S, Gunzner-Toste J, Hansen JD, Hatzivassiliou G, Liu B, Malesky K, Mathieu S, Newhouse B, Raddatz NJ, Ran Y, Rana S, Randolph N, Risom T, Rudolph J, Savage S, Selby LT, Shrag M, Song K, Sturgis HL, Voegtli WC, Wen Z, Willis BS, Woessner RD, Wu WI, Young WB, Grina J. Wenglowsky S, et al. Among authors: mathieu s. ACS Med Chem Lett. 2011 Mar 8;2(5):342-7. doi: 10.1021/ml200025q. eCollection 2011 May 12. ACS Med Chem Lett. 2011. PMID: 24900315 Free PMC article.
Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.
Crawford JJ, Lee W, Aliagas I, Mathieu S, Hoeflich KP, Zhou W, Wang W, Rouge L, Murray L, La H, Liu N, Fan PW, Cheong J, Heise CE, Ramaswamy S, Mintzer R, Liu Y, Chao Q, Rudolph J. Crawford JJ, et al. Among authors: mathieu s. J Med Chem. 2015 Jun 25;58(12):5121-36. doi: 10.1021/acs.jmedchem.5b00572. Epub 2015 Jun 12. J Med Chem. 2015. PMID: 26030457
Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight.
Touré BB, Giraldes J, Smith T, Sprague ER, Wang Y, Mathieu S, Chen Z, Mishina Y, Feng Y, Yan-Neale Y, Shakya S, Chen D, Meyer M, Puleo D, Brazell JT, Straub C, Sage D, Wright K, Yuan Y, Chen X, Duca J, Kim S, Tian L, Martin E, Hurov K, Shao W. Touré BB, et al. Among authors: mathieu s. J Med Chem. 2016 May 26;59(10):4711-23. doi: 10.1021/acs.jmedchem.6b00052. Epub 2016 May 17. J Med Chem. 2016. PMID: 27187609
363 results