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Page 1
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: quesnelle c. 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: quesnelle c. 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.
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: quesnelle c. 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
Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype.
Hill MD, Quesnelle C, Tokarski J, Fang H, Fanslau C, Haarhoff Z, Kramer M, Madari S, Wiebesiek A, Morrison J, Simmermacher-Mayer J, Sinz M, Westhouse R, Xie C, Zhao J, Huang L, Sheriff S, Yan C, Marsilio F, Everlof G, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: quesnelle c. Bioorg Med Chem Lett. 2021 Nov 1;51:128376. doi: 10.1016/j.bmcl.2021.128376. Epub 2021 Sep 21. Bioorg Med Chem Lett. 2021. PMID: 34560263
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
Hill MD, Fang H, Norris D, Delucca GV, Huang H, DeBenedetto M, Quesnelle C, Schmitz WD, Tokarski JS, Sheriff S, Yan C, Fanslau C, Haarhoff Z, Huang C, Kramer M, Madari S, Menard K, Monereau L, Morrison J, Raghavan N, Shields EE, Simmermacher-Mayer J, Sinz M, Tye CK, Westhouse R, Xie C, Zhang H, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: quesnelle c. ACS Med Chem Lett. 2022 Jul 5;13(7):1165-1171. doi: 10.1021/acsmedchemlett.2c00219. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859878 Free PMC article.
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: quesnelle c. 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
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: quesnelle c. J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816. J Med Chem. 2009. PMID: 19267461
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
Snyder LB, Meng Z, Mate R, D'Andrea SV, Marinier A, Quesnelle CA, Gill P, DenBleyker KL, Fung-Tomc JC, Frosco M, Martel A, Barrett JF, Bronson JJ. Snyder LB, et al. Among authors: quesnelle ca. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4735-9. doi: 10.1016/j.bmcl.2004.06.076. Bioorg Med Chem Lett. 2004. PMID: 15324898
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: quesnelle c. 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
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. 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
19 results