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Page 1
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Tian X, Suarez D, Thomson D, Li W, King EA, LaFrance L, Boehm J, Barton L, Di Marco C, Martyr C, Thalji R, Medina J, Knight S, Heerding D, Gao E, Nartey E, Cecconie T, Nixon C, Zhang G, Berrodin TJ, Phelps C, Patel A, Bai X, Lind K, Prabhu N, Messer J, Zhu Z, Shewchuk L, Reid R, Graves AP, McHugh C, Mangatt B. Tian X, et al. Among authors: thalji r. J Med Chem. 2022 Nov 10;65(21):14391-14408. doi: 10.1021/acs.jmedchem.2c00670. Epub 2022 Oct 27. J Med Chem. 2022. PMID: 36302181
Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement.
Barton LS, Callahan JF, Cantizani J, Concha NO, Cotillo Torrejon I, Goodwin NC, Joshi-Pangu A, Kiesow TJ, McAtee JJ, Mellinger M, Nixon CJ, Padrón-Barthe L, Patterson JR, Pearson ND, Pouliot JJ, Rendina AR, Buitrago Santanilla A, Schneck JL, Sanz O, Thalji RK, Ward P, Williams SP, King BW. Barton LS, et al. Among authors: thalji rk. Bioorg Med Chem. 2024 Feb 15;100:117618. doi: 10.1016/j.bmc.2024.117618. Epub 2024 Jan 29. Bioorg Med Chem. 2024. PMID: 38309201
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.
Thalji RK, Raha K, Andreotti D, Checchia A, Cui H, Meneghelli G, Profeta R, Tonelli F, Tommasi S, Bakshi T, Donovan BT, Howells A, Jain S, Nixon C, Quinque G, McCloskey L, Bax BD, Neu M, Chan PF, Stavenger RA. Thalji RK, et al. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1407-1412. doi: 10.1016/j.bmcl.2019.03.029. Epub 2019 Mar 22. Bioorg Med Chem Lett. 2019. PMID: 30962087
Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase.
Chan PF, Germe T, Bax BD, Huang J, Thalji RK, Bacqué E, Checchia A, Chen D, Cui H, Ding X, Ingraham K, McCloskey L, Raha K, Srikannathasan V, Maxwell A, Stavenger RA. Chan PF, et al. Among authors: thalji rk. Proc Natl Acad Sci U S A. 2017 May 30;114(22):E4492-E4500. doi: 10.1073/pnas.1700721114. Epub 2017 May 15. Proc Natl Acad Sci U S A. 2017. PMID: 28507124 Free PMC article.
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.
Thalji RK, McAtee JJ, Belyanskaya S, Brandt M, Brown GD, Costell MH, Ding Y, Dodson JW, Eisennagel SH, Fries RE, Gross JW, Harpel MR, Holt DA, Israel DI, Jolivette LJ, Krosky D, Li H, Lu Q, Mandichak T, Roethke T, Schnackenberg CG, Schwartz B, Shewchuk LM, Xie W, Behm DJ, Douglas SA, Shaw AL, Marino JP Jr. Thalji RK, et al. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3584-8. doi: 10.1016/j.bmcl.2013.04.019. Epub 2013 Apr 16. Bioorg Med Chem Lett. 2013. PMID: 23664879
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Morales-Ramos AI, Mecom JS, Kiesow TJ, Graybill TL, Brown GD, Aiyar NV, Davenport EA, Kallal LA, Knapp-Reed BA, Li P, Londregan AT, Morrow DM, Senadhi S, Thalji RK, Zhao S, Burns-Kurtis CL, Marino JP Jr. Morales-Ramos AI, et al. Among authors: thalji rk. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6222-6. doi: 10.1016/j.bmcl.2008.09.102. Epub 2008 Oct 2. Bioorg Med Chem Lett. 2008. PMID: 18926700
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.
Wang L, Sullivan GM, Hexamer LA, Hasvold LA, Thalji R, Przytulinska M, Tao ZF, Li G, Chen Z, Xiao Z, Gu WZ, Xue J, Bui MH, Merta P, Kovar P, Bouska JJ, Zhang H, Park C, Stewart KD, Sham HL, Sowin TJ, Rosenberg SH, Lin NH. Wang L, et al. Among authors: thalji r. J Med Chem. 2007 Aug 23;50(17):4162-76. doi: 10.1021/jm070105d. Epub 2007 Jul 21. J Med Chem. 2007. PMID: 17658776
18 results