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Page 1
Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates.
Li P, Dorsch W, Lauffer DJ, Bilimoria D, Chauret N, Court JJ, Das SK, Denis F, Mani N, Nanthakumar S, Nicolas O, Rao BG, Ronkin S, Selliah S, Shawgo RS, Stearns R, Tang Q, Waal ND, Green J. Li P, et al. Among authors: waal nd. ACS Med Chem Lett. 2017 Jan 31;8(2):251-255. doi: 10.1021/acsmedchemlett.6b00479. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197321 Free PMC article.
Discovery of Novel Thiophene-Based, Thumb Pocket 2 Allosteric Inhibitors of the Hepatitis C NS5B Polymerase with Improved Potency and Physicochemical Profiles.
Court JJ, Poisson C, Ardzinski A, Bilimoria D, Chan L, Chandupatla K, Chauret N, Collier PN, Das SK, Denis F, Dorsch W, Iyer G, Lauffer D, L'Heureux L, Li P, Luisi BS, Mani N, Nanthakumar S, Nicolas O, Rao BG, Ronkin S, Selliah S, Shawgo RS, Tang Q, Waal ND, Yannopoulos CG, Green J. Court JJ, et al. Among authors: waal nd. J Med Chem. 2016 Jul 14;59(13):6293-302. doi: 10.1021/acs.jmedchem.6b00541. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27366941
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Tang Q, Aronov AM, Deininger DD, Giroux S, Lauffer DJ, Li P, Liang J, McGinty K, Ronkin S, Swett R, Waal N, Boucher D, Ford PJ, Moody CS. Tang Q, et al. ACS Med Chem Lett. 2021 May 24;12(6):955-960. doi: 10.1021/acsmedchemlett.1c00094. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141080 Free PMC article.
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Grillot AL, Le Tiran A, Shannon D, Krueger E, Liao Y, O'Dowd H, Tang Q, Ronkin S, Wang T, Waal N, Li P, Lauffer D, Sizensky E, Tanoury J, Perola E, Grossman TH, Doyle T, Hanzelka B, Jones S, Dixit V, Ewing N, Liao S, Boucher B, Jacobs M, Bennani Y, Charifson PS. Grillot AL, et al. J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28. J Med Chem. 2014. PMID: 25317480
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Boyd MJ, Collier PN, Clark MP, Deng H, Kesavan S, Ronkin SM, Waal N, Wang J, Cao J, Li P, Come J, Davies I, Duffy JP, Cochran JE, Court JJ, Chandupatla K, Jackson KL, Maltais F, O'Dowd H, Boucher C, Considine T, Taylor WP, Gao H, Chakilam A, Engtrakul J, Crawford D, Doyle E, Phillips J, Kemper R, Swett R, Empfield J, Bunnage ME, Charifson PS, Magavi SS. Boyd MJ, et al. J Med Chem. 2021 Dec 23;64(24):17777-17794. doi: 10.1021/acs.jmedchem.1c00948. Epub 2021 Dec 6. J Med Chem. 2021. PMID: 34871500
Tethering identifies fragment that yields potent inhibitors of human caspase-1.
Fahr BT, O'Brien T, Pham P, Waal ND, Baskaran S, Raimundo BC, Lam JW, Sopko MM, Purkey HE, Romanowski MJ. Fahr BT, et al. Among authors: waal nd. Bioorg Med Chem Lett. 2006 Feb;16(3):559-62. doi: 10.1016/j.bmcl.2005.10.048. Epub 2005 Nov 4. Bioorg Med Chem Lett. 2006. PMID: 16274992
Structural analysis of caspase-1 inhibitors derived from Tethering.
O'Brien T, Fahr BT, Sopko MM, Lam JW, Waal ND, Raimundo BC, Purkey HE, Pham P, Romanowski MJ. O'Brien T, et al. Among authors: waal nd. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005 May 1;61(Pt 5):451-8. doi: 10.1107/S1744309105010109. Epub 2005 Apr 9. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005. PMID: 16511067 Free PMC article.