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Page 1
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, Waterson AG, Dickerson SH, Mook RA Jr, Laquerre SG, King AJ, Rossanese OW, Arnone MR, Smitheman KN, Kane-Carson LS, Han C, Moorthy GS, Moss KG, Uehling DE. Rheault TR, et al. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. doi: 10.1021/ml4000063. eCollection 2013 Mar 14. ACS Med Chem Lett. 2013. PMID: 24900673 Free PMC article.
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA Jr, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE. Stellwagen JC, et al. Among authors: rheault tr. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021. Epub 2011 Jun 16. Bioorg Med Chem Lett. 2011. PMID: 21733693
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
Stevens KL, Alligood KJ, Alberti JG, Caferro TR, Chamberlain SD, Dickerson SH, Dickson HD, Emerson HK, Griffin RJ, Hubbard RD, Keith BR, Mullin RJ, Petrov KG, Gerding RM, Reno MJ, Rheault TR, Rusnak DW, Sammond DM, Smith SC, Uehling DE, Waterson AG, Wood ER. Stevens KL, et al. Among authors: rheault tr. Bioorg Med Chem Lett. 2009 Jan 1;19(1):21-6. doi: 10.1016/j.bmcl.2008.11.023. Epub 2008 Nov 13. Bioorg Med Chem Lett. 2009. PMID: 19028424
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.
Rheault TR, Caferro TR, Dickerson SH, Donaldson KH, Gaul MD, Goetz AS, Mullin RJ, McDonald OB, Petrov KG, Rusnak DW, Shewchuk LM, Spehar GM, Truesdale AT, Vanderwall DE, Wood ER, Uehling DE. Rheault TR, et al. Bioorg Med Chem Lett. 2009 Feb 1;19(3):817-20. doi: 10.1016/j.bmcl.2008.12.011. Epub 2008 Dec 7. Bioorg Med Chem Lett. 2009. PMID: 19111461
Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions.
King AJ, Arnone MR, Bleam MR, Moss KG, Yang J, Fedorowicz KE, Smitheman KN, Erhardt JA, Hughes-Earle A, Kane-Carson LS, Sinnamon RH, Qi H, Rheault TR, Uehling DE, Laquerre SG. King AJ, et al. Among authors: rheault tr. PLoS One. 2013 Jul 3;8(7):e67583. doi: 10.1371/journal.pone.0067583. Print 2013. PLoS One. 2013. PMID: 23844038 Free PMC article.
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.
Becherer JD, Boros EE, Carpenter TY, Cowan DJ, Deaton DN, Haffner CD, Jeune MR, Kaldor IW, Poole JC, Preugschat F, Rheault TR, Schulte CA, Shearer BG, Shearer TW, Shewchuk LM, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC. Becherer JD, et al. Among authors: rheault tr. J Med Chem. 2015 Sep 10;58(17):7021-56. doi: 10.1021/acs.jmedchem.5b00992. Epub 2015 Aug 24. J Med Chem. 2015. PMID: 26267483
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