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Page 1
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.
Palmer WS, Alam M, Arzeno HB, Chang KC, Dunn JP, Goldstein DM, Gong L, Goyal B, Hermann JC, Hogg JH, Hsieh G, Jahangir A, Janson C, Jin S, Ursula Kammlott R, Kuglstatter A, Lukacs C, Michoud C, Niu L, Reuter DC, Shao A, Silva T, Trejo-Martin TA, Stein K, Tan YC, Tivitmahaisoon P, Tran P, Wagner P, Weller P, Wu SY. Palmer WS, et al. Among authors: tan yc. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1486-92. doi: 10.1016/j.bmcl.2012.12.047. Epub 2012 Dec 22. Bioorg Med Chem Lett. 2013. PMID: 23352510
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. 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 a novel series of 4-quinolone JNK inhibitors.
Gong L, Tan YC, Boice G, Abbot S, McCaleb K, Iyer P, Zuo F, Dal Porto J, Wong B, Jin S, Chang A, Tran P, Hsieh G, Niu L, Shao A, Reuter D, Lukacs CM, Ursula Kammlott R, Kuglstatter A, Goldstein D. Gong L, et al. Among authors: tan yc. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7381-7. doi: 10.1016/j.bmcl.2012.10.066. Epub 2012 Oct 24. Bioorg Med Chem Lett. 2012. PMID: 23142618
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.
Gong L, Han X, Silva T, Tan YC, Goyal B, Tivitmahaisoon P, Trejo A, Palmer W, Hogg H, Jahagir A, Alam M, Wagner P, Stein K, Filonova L, Loe B, Makra F, Rotstein D, Rapatova L, Dunn J, Zuo F, Dal Porto J, Wong B, Jin S, Chang A, Tran P, Hsieh G, Niu L, Shao A, Reuter D, Hermann J, Kuglstatter A, Goldstein D. Gong L, et al. Among authors: tan yc. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3565-9. doi: 10.1016/j.bmcl.2013.04.029. Epub 2013 Apr 21. Bioorg Med Chem Lett. 2013. PMID: 23664880
Discovery of potent and bioavailable GSK-3beta inhibitors.
Gong L, Hirschfeld D, Tan YC, Heather Hogg J, Peltz G, Avnur Z, Dunten P. Gong L, et al. Among authors: tan yc. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1693-6. doi: 10.1016/j.bmcl.2010.01.038. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20138512
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villaseñor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC. Padilla F, et al. Among authors: tan yc. J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12. J Med Chem. 2013. PMID: 23350847
Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase.
Talamas FX, Abbot SC, Anand S, Brameld KA, Carter DS, Chen J, Davis D, de Vicente J, Fung AD, Gong L, Harris SF, Inbar P, Labadie SS, Lee EK, Lemoine R, Le Pogam S, Leveque V, Li J, McIntosh J, Nájera I, Park J, Railkar A, Rajyaguru S, Sangi M, Schoenfeld RC, Staben LR, Tan Y, Taygerly JP, Villaseñor AG, Weller PE. Talamas FX, et al. J Med Chem. 2014 Mar 13;57(5):1914-31. doi: 10.1021/jm401329s. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24195700 Free PMC article.
At-admission prediction of mortality and pulmonary embolism in an international cohort of hospitalised patients with COVID-19 using statistical and machine learning methods.
Mesinovic M, Wong XC, Rajahram GS, Citarella BW, Peariasamy KM, van Someren Greve F, Olliaro P, Merson L, Clifton L, Kartsonaki C; ISARIC Characterisation Group. Mesinovic M, et al. Sci Rep. 2024 Jul 16;14(1):16387. doi: 10.1038/s41598-024-63212-7. Sci Rep. 2024. PMID: 39013928 Free PMC article.
212 results