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Page 1
Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.
Weinberg LR, Albom MS, Angeles TS, Husten J, Lisko JG, McHugh RJ, Milkiewicz KL, Murthy S, Ott GR, Theroff JP, Tripathy R, Underiner TL, Zificsak CA, Dorsey BD. Weinberg LR, et al. Among authors: theroff jp. Bioorg Med Chem Lett. 2011 Jan 1;21(1):164-7. doi: 10.1016/j.bmcl.2010.11.045. Epub 2010 Nov 11. Bioorg Med Chem Lett. 2011. PMID: 21123062
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.
Zificsak CA, Theroff JP, Aimone LD, Albom MS, Angeles TS, Brown RA, Galinis D, Grobelny JV, Herbertz T, Husten J, Kocsis LS, LoSardo C, Miknyoczki SJ, Murthy S, Rolon-Steele D, Underiner TL, Wells-Knecht KJ, Worrell CS, Zeigler KS, Dorsey BD. Zificsak CA, et al. Among authors: theroff jp. Bioorg Med Chem Lett. 2011 Jan 15;21(2):660-3. doi: 10.1016/j.bmcl.2010.12.013. Epub 2010 Dec 8. Bioorg Med Chem Lett. 2011. PMID: 21190849
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA, Dorsey BD. Milkiewicz KL, et al. Among authors: theroff jp. Bioorg Med Chem. 2010 Jun 15;18(12):4351-62. doi: 10.1016/j.bmc.2010.04.087. Epub 2010 Apr 29. Bioorg Med Chem. 2010. PMID: 20483621
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.
Soth MJ, Le K, Di Francesco ME, Hamilton MM, Liu G, Burke JP, Carroll CL, Kovacs JJ, Bardenhagen JP, Bristow CA, Cardozo M, Czako B, de Stanchina E, Feng N, Garvey JR, Gay JP, Do MKG, Greer J, Han M, Harris A, Herrera Z, Huang S, Giuliani V, Jiang Y, Johnson SB, Johnson TA, Kang Z, Leonard PG, Liu Z, McAfoos T, Miller M, Morlacchi P, Mullinax RA, Palmer WS, Pang J, Rogers N, Rudin CM, Shepard HE, Spencer ND, Theroff J, Wu Q, Xu A, Yau JA, Draetta G, Toniatti C, Heffernan TP, Jones P. Soth MJ, et al. Among authors: theroff j. J Med Chem. 2020 Nov 12;63(21):12957-12977. doi: 10.1021/acs.jmedchem.0c01398. Epub 2020 Oct 29. J Med Chem. 2020. PMID: 33118821 Free PMC article.
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.
Zificsak CA, Gingrich DE, Breslin HJ, Dunn DD, Milkiewicz KL, Theroff JP, Thieu TV, Underiner TL, Weinberg LR, Aimone LD, Albom MS, Mason JL, Saville L, Husten J, Angeles TS, Finn JP, Jan M, O'Kane TM, Dobrzanski P, Dorsey BD. Zificsak CA, et al. Among authors: theroff jp. Bioorg Med Chem Lett. 2012 Jan 1;22(1):133-7. doi: 10.1016/j.bmcl.2011.11.049. Epub 2011 Nov 25. Bioorg Med Chem Lett. 2012. PMID: 22169263
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: theroff jp. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.
Palmer WS, Poncet-Montange G, Liu G, Petrocchi A, Reyna N, Subramanian G, Theroff J, Yau A, Kost-Alimova M, Bardenhagen JP, Leo E, Shepard HE, Tieu TN, Shi X, Zhan Y, Zhao S, Barton MC, Draetta G, Toniatti C, Jones P, Geck Do M, Andersen JN. Palmer WS, et al. Among authors: theroff j. J Med Chem. 2016 Feb 25;59(4):1440-54. doi: 10.1021/acs.jmedchem.5b00405. Epub 2015 Jul 6. J Med Chem. 2016. PMID: 26061247 Free PMC article.
13 results