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Page 1
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Bregman H, Chakka N, Guzman-Perez A, Gunaydin H, Gu Y, Huang X, Berry V, Liu J, Teffera Y, Huang L, Egge B, Mullady EL, Schneider S, Andrews PS, Mishra A, Newcomb J, Serafino R, Strathdee CA, Turci SM, Wilson C, DiMauro EF. Bregman H, et al. J Med Chem. 2013 Jun 13;56(11):4320-42. doi: 10.1021/jm4000038. Epub 2013 May 23. J Med Chem. 2013. PMID: 23701517
Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.
Hua Z, Bregman H, Buchanan JL, Chakka N, Guzman-Perez A, Gunaydin H, Huang X, Gu Y, Berry V, Liu J, Teffera Y, Huang L, Egge B, Emkey R, Mullady EL, Schneider S, Andrews PS, Acquaviva L, Dovey J, Mishra A, Newcomb J, Saffran D, Serafino R, Strathdee CA, Turci SM, Stanton M, Wilson C, Dimauro EF. Hua Z, et al. J Med Chem. 2013 Dec 27;56(24):10003-15. doi: 10.1021/jm401317z. Epub 2013 Dec 11. J Med Chem. 2013. PMID: 24294969
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S. Schenkel LB, et al. J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4. J Med Chem. 2016. PMID: 26942860
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Bojic EF, Foti RS, Fremeau R, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, Kornecook T, Lee J, Ligutti J, Liu D, Moyer BD, Ortuno D, Rose PE, Schenkel LB, Taborn K, Wang J, Wang Y, Yu V, Weiss MM. DiMauro EF, et al. J Med Chem. 2016 Sep 8;59(17):7818-39. doi: 10.1021/acs.jmedchem.6b00425. Epub 2016 Aug 29. J Med Chem. 2016. PMID: 27441383
Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors.
Schenkel LB, DiMauro EF, Nguyen HN, Chakka N, Du B, Foti RS, Guzman-Perez A, Jarosh M, La DS, Ligutti J, Milgram BC, Moyer BD, Peterson EA, Roberts J, Yu VL, Weiss MM. Schenkel LB, et al. Among authors: guzman perez a. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3817-3824. doi: 10.1016/j.bmcl.2017.06.054. Epub 2017 Jun 26. Bioorg Med Chem Lett. 2017. PMID: 28684121
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, Plant MH, Shaffer PL, Teffera Y, Yi S, Zhang M, Gingras J, DiMauro EF. Bregman H, et al. J Med Chem. 2017 Feb 9;60(3):1105-1125. doi: 10.1021/acs.jmedchem.6b01496. Epub 2016 Dec 21. J Med Chem. 2017. PMID: 28001399
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr. Weiss MM, et al. J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28287723
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss MM. Graceffa RF, et al. J Med Chem. 2017 Jul 27;60(14):5990-6017. doi: 10.1021/acs.jmedchem.6b01850. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28324649
46 results