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19 results

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Page 1
Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.
Tanis SP, Plewe MB, Johnson TW, Butler SL, Dalvie D, DeLisle D, Dress KR, Hu Q, Huang B, Kuehler JE, Kuki A, Liu W, Peng Q, Smith GL, Solowiej J, Tran KT, Wang H, Yang A, Yin C, Yu X, Zhang J, Zhu H. Tanis SP, et al. Among authors: solowiej j. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7429-34. doi: 10.1016/j.bmcl.2010.10.022. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21036042
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Johnson TW, Tanis SP, Butler SL, Dalvie D, Delisle DM, Dress KR, Flahive EJ, Hu Q, Kuehler JE, Kuki A, Liu W, McClellan GA, Peng Q, Plewe MB, Richardson PF, Smith GL, Solowiej J, Tran KT, Wang H, Yu X, Zhang J, Zhu H. Johnson TW, et al. Among authors: solowiej j. J Med Chem. 2011 May 12;54(9):3393-417. doi: 10.1021/jm200208d. Epub 2011 Apr 13. J Med Chem. 2011. PMID: 21446745
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.
Freeman-Cook KD, Hoffman RL, Behenna DC, Boras B, Carelli J, Diehl W, Ferre RA, He YA, Hui A, Huang B, Huser N, Jones R, Kephart SE, Lapek J, McTigue M, Miller N, Murray BW, Nagata A, Nguyen L, Niessen S, Ninkovic S, O'Doherty I, Ornelas MA, Solowiej J, Sutton SC, Tran K, Tseng E, Visswanathan R, Xu M, Zehnder L, Zhang Q, Zhang C, Dann S. Freeman-Cook KD, et al. Among authors: solowiej j. J Med Chem. 2021 Jul 8;64(13):9056-9077. doi: 10.1021/acs.jmedchem.1c00159. Epub 2021 Jun 10. J Med Chem. 2021. PMID: 34110834
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC. Cheng H, et al. Among authors: solowiej j. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. J Med Chem. 2016. PMID: 26756222
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM, Edwards MP, Ferre RA, Gajiwala KS, Hemkens M, Kania RS, Kath JC, Matthews J, Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin S, Zhang C, Lafontaine J. Planken S, et al. Among authors: solowiej j. J Med Chem. 2017 Apr 13;60(7):3002-3019. doi: 10.1021/acs.jmedchem.6b01894. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28287730
Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance.
Schwartz PA, Kuzmic P, Solowiej J, Bergqvist S, Bolanos B, Almaden C, Nagata A, Ryan K, Feng J, Dalvie D, Kath JC, Xu M, Wani R, Murray BW. Schwartz PA, et al. Among authors: solowiej j. Proc Natl Acad Sci U S A. 2014 Jan 7;111(1):173-8. doi: 10.1073/pnas.1313733111. Epub 2013 Dec 17. Proc Natl Acad Sci U S A. 2014. PMID: 24347635 Free PMC article.
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Hoffman RL, Kania RS, Brothers MA, Davies JF, Ferre RA, Gajiwala KS, He M, Hogan RJ, Kozminski K, Li LY, Lockner JW, Lou J, Marra MT, Mitchell LJ Jr, Murray BW, Nieman JA, Noell S, Planken SP, Rowe T, Ryan K, Smith GJ 3rd, Solowiej JE, Steppan CM, Taggart B. Hoffman RL, et al. Among authors: solowiej je. J Med Chem. 2020 Nov 12;63(21):12725-12747. doi: 10.1021/acs.jmedchem.0c01063. Epub 2020 Oct 15. J Med Chem. 2020. PMID: 33054210
Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor.
Freeman-Cook K, Hoffman RL, Miller N, Almaden J, Chionis J, Zhang Q, Eisele K, Liu C, Zhang C, Huser N, Nguyen L, Costa-Jones C, Niessen S, Carelli J, Lapek J, Weinrich SL, Wei P, McMillan E, Wilson E, Wang TS, McTigue M, Ferre RA, He YA, Ninkovic S, Behenna D, Tran KT, Sutton S, Nagata A, Ornelas MA, Kephart SE, Zehnder LR, Murray B, Xu M, Solowiej JE, Visswanathan R, Boras B, Looper D, Lee N, Bienkowska JR, Zhu Z, Kan Z, Ding Y, Mu XJ, Oderup C, Salek-Ardakani S, White MA, VanArsdale T, Dann SG. Freeman-Cook K, et al. Among authors: solowiej je. Cancer Cell. 2021 Oct 11;39(10):1404-1421.e11. doi: 10.1016/j.ccell.2021.08.009. Epub 2021 Sep 13. Cancer Cell. 2021. PMID: 34520734 Free article.
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