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Page 1
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, Malek S, Peterson D, Pitts KE, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A. Dragovich PS, et al. Among authors: robarge k. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3764-71. doi: 10.1016/j.bmcl.2014.06.076. Epub 2014 Jul 1. Bioorg Med Chem Lett. 2014. PMID: 25037916
Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P, Burton B, Choo EF, Pang J, Boggs J, Yang A, Yang X, Baumgardner M. Robarge KD, et al. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723. doi: 10.1016/j.bmcl.2014.08.008. Epub 2014 Aug 15. Bioorg Med Chem Lett. 2014. PMID: 25193232
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Labadie S, Dragovich PS, Chen J, Fauber BP, Boggs J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Ho Q, Lai KW, Ma S, Malek S, Peterson D, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A. Labadie S, et al. Among authors: robarge k. Bioorg Med Chem Lett. 2015 Jan 1;25(1):75-82. doi: 10.1016/j.bmcl.2014.11.008. Epub 2014 Nov 10. Bioorg Med Chem Lett. 2015. PMID: 25466195
Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.
Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Labadie S, Malek S, Peterson D, Purkey HE, Robarge K, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhou A. Fauber BP, et al. Among authors: robarge k. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5683-5687. doi: 10.1016/j.bmcl.2014.10.067. Epub 2014 Oct 27. Bioorg Med Chem Lett. 2014. PMID: 25467161
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.
Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, Labadie SS, Lai KW, Liu W, Liu Y, Li C, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhang H, Zhou A. Purkey HE, et al. Among authors: robarge k. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. doi: 10.1021/acsmedchemlett.6b00190. eCollection 2016 Oct 13. ACS Med Chem Lett. 2016. PMID: 27774125 Free PMC article.
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Wei B, Robarge K, Labadie SS, Chen J, Corson LB, DiPasquale A, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Hitz A, Hong R, Lai KW, Liu W, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Ultsch M, Xu Z, Yen I, Yu D, Yue Q, Zhou A, Purkey HE. Wei B, et al. Among authors: robarge k. Bioorg Med Chem Lett. 2022 Mar 1;59:128576. doi: 10.1016/j.bmcl.2022.128576. Epub 2022 Jan 19. Bioorg Med Chem Lett. 2022. PMID: 35065235
Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.
Castanedo GM, Wang S, Robarge KD, Blackwood E, Burdick D, Chang C, Dijkgraaf GJ, Gould S, Gunzner J, Guichert O, Halladay J, Khojasteh C, Lee L, Marsters JC Jr, Murray L, Peterson D, Plise E, Salphati L, de Sauvage FJ, Wong S, Sutherlin DP. Castanedo GM, et al. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6748-53. doi: 10.1016/j.bmcl.2010.08.134. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20875741
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.
Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP. Cohen F, et al. Among authors: robarge kd. J Med Chem. 2011 May 12;54(9):3426-35. doi: 10.1021/jm200215y. Epub 2011 Apr 15. J Med Chem. 2011. PMID: 21495671
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Fauber BP, Gobbi A, Robarge K, Zhou A, Barnard A, Cao J, Deng Y, Eidenschenk C, Everett C, Ganguli A, Hawkins J, Johnson AR, La H, Norman M, Salmon G, Summerhill S, Ouyang W, Tang W, Wong H. Fauber BP, et al. Among authors: robarge k. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2907-12. doi: 10.1016/j.bmcl.2015.05.055. Epub 2015 May 28. Bioorg Med Chem Lett. 2015. PMID: 26048793
23 results