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Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif.
Filipski KJ, Guzman-Perez A, Bian J, Perreault C, Aspnes GE, Didiuk MT, Dow RL, Hank RF, Jones CS, Maguire RJ, Tu M, Zeng D, Liu S, Knafels JD, Litchfield J, Atkinson K, Derksen DR, Bourbonais F, Gajiwala KS, Hickey M, Johnson TO, Humphries PS, Pfefferkorn JA. Filipski KJ, et al. Among authors: gajiwala ks. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4571-8. doi: 10.1016/j.bmcl.2013.06.036. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23831135
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide.
Zehnder L, Bennett M, Meng J, Huang B, Ninkovic S, Wang F, Braganza J, Tatlock J, Jewell T, Zhou JZ, Burke B, Wang J, Maegley K, Mehta PP, Yin MJ, Gajiwala KS, Hickey MJ, Yamazaki S, Smith E, Kang P, Sistla A, Dovalsantos E, Gehring MR, Kania R, Wythes M, Kung PP. Zehnder L, et al. Among authors: gajiwala ks. J Med Chem. 2011 May 12;54(9):3368-85. doi: 10.1021/jm200128m. Epub 2011 Apr 20. J Med Chem. 2011. PMID: 21438541
SAH derived potent and selective EZH2 inhibitors.
Kung PP, Huang B, Zehnder L, Tatlock J, Bingham P, Krivacic C, Gajiwala K, Diehl W, Yu X, Maegley KA. Kung PP, et al. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1532-7. doi: 10.1016/j.bmcl.2015.02.017. Epub 2015 Feb 17. Bioorg Med Chem Lett. 2015. PMID: 25746813
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: gajiwala ks. 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
Solution-phase parallel synthesis of Hsp90 inhibitors.
Cho-Schultz S, Patten MJ, Huang B, Elleraas J, Gajiwala KS, Hickey MJ, Wang J, Mehta PP, Kang P, Gehring MR, Kung PP, Sutton SC. Cho-Schultz S, et al. Among authors: gajiwala ks. J Comb Chem. 2009 Sep-Oct;11(5):860-74. doi: 10.1021/cc900056d. J Comb Chem. 2009. PMID: 19583220
Ack1: activation and regulation by allostery.
Gajiwala KS, Maegley K, Ferre R, He YA, Yu X. Gajiwala KS, et al. PLoS One. 2013;8(1):e53994. doi: 10.1371/journal.pone.0053994. Epub 2013 Jan 14. PLoS One. 2013. PMID: 23342057 Free PMC article.
40 results