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378 results

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Page 1
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z. Papillon JPN, et al. Among authors: mathieu s. J Med Chem. 2018 Nov 21;61(22):10155-10172. doi: 10.1021/acs.jmedchem.8b01318. Epub 2018 Oct 31. J Med Chem. 2018. PMID: 30339381
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
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
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
The Discovery of SWI/SNF Chromatin Remodeling Activity as a Novel and Targetable Dependency in Uveal Melanoma.
Rago F, Elliott G, Li A, Sprouffske K, Kerr G, Desplat A, Abramowski D, Chen JT, Farsidjani A, Xiang KX, Bushold G, Feng Y, Shirley MD, Bric A, Vattay A, Möbitz H, Nakajima K, Adair CD, Mathieu S, Ntaganda R, Smith T, Papillon JPN, Kauffmann A, Ruddy DA, Bhang HC, Castelletti D, Jagani Z. Rago F, et al. Among authors: mathieu s. Mol Cancer Ther. 2020 Oct;19(10):2186-2195. doi: 10.1158/1535-7163.MCT-19-1013. Epub 2020 Aug 3. Mol Cancer Ther. 2020. PMID: 32747420
378 results