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Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.
Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA. Marcin LR, et al. Among authors: kopcho lm. Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079. Bioorg Med Chem Lett. 2011. PMID: 21078556
Development of a RapidFire mass spectrometry assay and a fluorescence assay for the discovery of kynurenine aminotransferase II inhibitors to treat central nervous system disorders.
Lu H, Kopcho L, Ghosh K, Witmer M, Parker M, Gupta S, Paul M, Krishnamurthy P, Laksmaiah B, Xie D, Tredup J, Zhang L, Abell LM. Lu H, et al. Among authors: kopcho l. Anal Biochem. 2016 May 15;501:56-65. doi: 10.1016/j.ab.2016.02.003. Epub 2016 Feb 11. Anal Biochem. 2016. PMID: 26874021
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.
Xiao HY, Li N, Duan JJ, Jiang B, Lu Z, Ngu K, Tino J, Kopcho LM, Lu H, Chen J, Tebben AJ, Sheriff S, Chang CY, Yanchunas J Jr, Calambur D, Gao M, Shuster DJ, Susulic V, Xie JH, Guarino VR, Wu DR, Gregor KR, Goldstine CB, Hynes J Jr, Macor JE, Salter-Cid L, Burke JR, Shaw PJ, Dhar TGM. Xiao HY, et al. Among authors: kopcho lm. J Med Chem. 2020 Dec 10;63(23):15050-15071. doi: 10.1021/acs.jmedchem.0c01732. Epub 2020 Dec 1. J Med Chem. 2020. PMID: 33261314
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.
Zhang L, Cherney EC, Zhu X, Lin TA, Gullo-Brown J, Maley D, Johnston-Allegretto K, Kopcho L, Fereshteh M, Huang C, Li X, Traeger SC, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan T, Borzilleri R, Vite G, Hunt JT, Balog A. Zhang L, et al. ACS Med Chem Lett. 2021 Mar 2;12(3):494-501. doi: 10.1021/acsmedchemlett.1c00014. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738077 Free PMC article.
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Cherney EC, Zhang L, Nara S, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, Darienzo C, Discenza L, Ranasinghe A, Grubb M, Ziemba T, Traeger SC, Li X, Johnston K, Kopcho L, Fereshteh M, Foster K, Stefanski K, Fargnoli J, Swanson J, Brown J, Delpy D, Seitz SP, Borzilleri R, Vite G, Balog A. Cherney EC, et al. ACS Med Chem Lett. 2021 Jan 28;12(2):288-294. doi: 10.1021/acsmedchemlett.0c00668. eCollection 2021 Feb 11. ACS Med Chem Lett. 2021. PMID: 33603977 Free PMC article.
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Cherney EC, Zhang L, Guo W, Huang A, Williams D, Seitz S, Shan W, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, D'Arienzo CJ, Discenza LN, Ranasinghe A, Grubb MF, Traeger SC, Li X, Johnston KA, Kopcho L, Fereshteh M, Foster KA, Stefanski K, Delpy D, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan TT, Pattasseri S, Nimje RY, Hong Z, Kempson J, Rampulla R, Mathur A, Gupta A, Borzilleri R, Vite G, Balog A. Cherney EC, et al. ACS Med Chem Lett. 2021 Jun 16;12(7):1143-1150. doi: 10.1021/acsmedchemlett.1c00236. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267885 Free PMC article.
Potent Triazolopyridine Myeloperoxidase Inhibitors.
Wurtz NR, Viet A, Shaw SA, Dilger A, Valente MN, Khan JA, Jusuf S, Narayanan R, Fernando G, Lo F, Liu X, Locke GA, Kopcho L, Abell LM, Sleph P, Basso M, Zhao L, Wexler RR, Duclos F, Kick EK. Wurtz NR, et al. Among authors: kopcho l. ACS Med Chem Lett. 2018 Nov 1;9(12):1175-1180. doi: 10.1021/acsmedchemlett.8b00308. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613322 Free PMC article.
29 results