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Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML, Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H. Goldstein DM, et al. Among authors: graves b. J Med Chem. 2011 Apr 14;54(7):2255-65. doi: 10.1021/jm101423y. Epub 2011 Mar 4. J Med Chem. 2011. PMID: 21375264
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Chu XJ, et al. Among authors: graves b. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B. Ding Q, et al. Among authors: graves b. J Med Chem. 2013 Jul 25;56(14):5979-83. doi: 10.1021/jm400487c. Epub 2013 Jul 16. J Med Chem. 2013. PMID: 23808545
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.
Zhang Z, Chu XJ, Liu JJ, Ding Q, Zhang J, Bartkovitz D, Jiang N, Karnachi P, So SS, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev L, Graves B. Zhang Z, et al. Among authors: graves b. ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. doi: 10.1021/ml400359z. eCollection 2014 Feb 13. ACS Med Chem Lett. 2013. PMID: 24900784 Free PMC article.
Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development.
Guerlavais V, Sawyer TK, Carvajal L, Chang YS, Graves B, Ren JG, Sutton D, Olson KA, Packman K, Darlak K, Elkin C, Feyfant E, Kesavan K, Gangurde P, Vassilev LT, Nash HM, Vukovic V, Aivado M, Annis DA. Guerlavais V, et al. Among authors: graves b. J Med Chem. 2023 Jul 27;66(14):9401-9417. doi: 10.1021/acs.jmedchem.3c00623. Epub 2023 Jul 13. J Med Chem. 2023. PMID: 37439511
Concepts and progress in the development of peptide mimetics.
Olson GL, Bolin DR, Bonner MP, Bös M, Cook CM, Fry DC, Graves BJ, Hatada M, Hill DE, Kahn M, et al. Olson GL, et al. Among authors: graves bj. J Med Chem. 1993 Oct 15;36(21):3039-49. doi: 10.1021/jm00073a001. J Med Chem. 1993. PMID: 8230089 Review. No abstract available.
Small molecule inhibitors of p53/MDM2 interaction.
Fotouhi N, Graves B. Fotouhi N, et al. Among authors: graves b. Curr Top Med Chem. 2005;5(2):159-65. doi: 10.2174/1568026053507705. Curr Top Med Chem. 2005. PMID: 15853644 Review.
326 results