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Page 1
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. Among authors: gill p. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
Sordaricin antifungal agents.
Quesnelle CA, Gill P, Dodier M, St Laurent D, Serrano-Wu M, Marinier A, Martel A, Mazzucco CE, Stickle TM, Barrett JF, Vyas DM, Balasubramanian BN. Quesnelle CA, et al. Among authors: gill p. Bioorg Med Chem Lett. 2003 Feb 10;13(3):519-24. doi: 10.1016/s0960-894x(02)00937-x. Bioorg Med Chem Lett. 2003. PMID: 12565963
Identification of a broad-spectrum azasordarin with improved pharmacokinetic properties.
Serrano-Wu MH, Laurent DR, Carroll TM, Dodier M, Gao Q, Gill P, Quesnelle C, Marinier A, Mazzucco CE, Regueiro-Ren A, Stickle TM, Wu D, Yang H, Yang Z, Zheng M, Zoeckler ME, Vyas DM, Balasubramanian BN. Serrano-Wu MH, et al. Among authors: gill p. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1419-23. doi: 10.1016/s0960-894x(03)00161-6. Bioorg Med Chem Lett. 2003. PMID: 12668003
Biaryl isoxazolinone antibacterial agents.
Quesnelle CA, Gill P, Roy S, Dodier M, Marinier A, Martel A, Snyder LB, D'Andrea SV, Bronson JJ, Frosco M, Beaulieu D, Warr GA, Denbleyker KL, Stickle TM, Yang H, Chaniewski SE, Ferraro CA, Taylor D, Russell JW, Santone KS, Clarke J, Drain RL, Knipe JO, Mosure K, Barrett JF. Quesnelle CA, et al. Among authors: gill p. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2728-33. doi: 10.1016/j.bmcl.2005.04.003. Bioorg Med Chem Lett. 2005. PMID: 15869878
Novel tricyclic inhibitors of IkappaB kinase.
Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Kempson J, et al. Among authors: gill p. J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816. J Med Chem. 2009. PMID: 19267461
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Dyckman AJ, et al. Among authors: gill p. Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21087862
BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.
Shan W, Balog A, Quesnelle C, Gill P, Han WC, Norris D, Mandal S, Thiruvenkadam R, Gona KB, Thiyagarajan K, Kandula S, McGlinchey K, Menard K, Wen ML, Rose A, White R, Guarino V, Shen DR, Cvijic ME, Ranasinghe A, Dai J, Zhang Y, Wu DR, Mathur A, Rampulla R, Trainor G, Hunt JT, Vite GD, Westhouse R, Lee FY, Gavai AV. Shan W, et al. Among authors: gill p. Bioorg Med Chem Lett. 2015 May 1;25(9):1905-9. doi: 10.1016/j.bmcl.2015.03.038. Epub 2015 Mar 23. Bioorg Med Chem Lett. 2015. PMID: 25857941
Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors.
Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY. Gavai AV, et al. Among authors: gill p. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7. doi: 10.1021/acsmedchemlett.5b00001. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005526 Free PMC article.
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.
Harikrishnan LS, Gill P, Kamau MG, Qin LY, Ruan Z, O'Malley D, Huynh T, Stachura S, Cavallaro CL, Lu Z, J-W Duan J, Weigelt CA, Sack JS, Ruzanov M, Khan J, Gururajan M, Wong JJ, Huang Y, Yarde M, Li Z, Chen C, Sun H, Borowski V, Murtaza A, Fink BE. Harikrishnan LS, et al. Among authors: gill p. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127204. doi: 10.1016/j.bmcl.2020.127204. Epub 2020 Apr 20. Bioorg Med Chem Lett. 2020. PMID: 32334911
1,947 results