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Page 1
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM. Wittman MD, et al. Among authors: menard k. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.
Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, Hillerman S, Cao C, Cantor GH, Dell-John J, Chen C, Discenza L, Menard K, Li A, Trainor G, Vyas D, Kramer R, Attar RM, Gottardis MM. Carboni JM, et al. Among authors: menard k. Mol Cancer Ther. 2009 Dec;8(12):3341-9. doi: 10.1158/1535-7163.MCT-09-0499. Mol Cancer Ther. 2009. PMID: 19996272
Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Velaparthi U, Saulnier MG, Wittman MD, Liu P, Frennesson DB, Zimmermann K, Carboni JM, Gottardis M, Li A, Greer A, Clarke W, Yang Z, Menard K, Lee FY, Trainor G, Vyas D. Velaparthi U, et al. Among authors: menard k. Bioorg Med Chem Lett. 2010 May 15;20(10):3182-5. doi: 10.1016/j.bmcl.2010.03.057. Epub 2010 Mar 27. Bioorg Med Chem Lett. 2010. PMID: 20399649
Biochemical and transcriptional profiling to triage additional activities in a series of IGF-1R/IR inhibitors.
Ross-Macdonald P, de Silva H, Patel V, Truong A, He A, Neuhaus I, Tilford C, Ji R, Siemers N, Greer A, Carboni J, Gottardis M, Menard K, Lee F, Dodier M, Frennesson D, Sampognaro A, Saulnier M, Trainor G, Vyas D, Zimmermann K, Wittman M. Ross-Macdonald P, et al. Among authors: menard k. Bioorg Med Chem. 2012 Mar 15;20(6):1961-72. doi: 10.1016/j.bmc.2011.10.090. Epub 2011 Nov 6. Bioorg Med Chem. 2012. PMID: 22137930
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: menard k. 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: menard k. 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: menard k. 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 search for structural diversity.
Hill MD, Fang H, Tokarski J, Fanslau C, Haarhoff Z, Huang C, Kramer M, Menard K, Monereau L, Morrison J, Ranasinghe A, Shields EE, Tye CK, Westhouse R, Everlof G, Sheriff S, Yan C, Marsilio F, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: menard k. Bioorg Med Chem Lett. 2021 Jul 15;44:128108. doi: 10.1016/j.bmcl.2021.128108. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991625
Preclinical efficacy spectrum and pharmacokinetics of ixabepilone.
Lee FY, Smykla R, Johnston K, Menard K, McGlinchey K, Peterson RW, Wiebesiek A, Vite G, Fairchild CR, Kramer R. Lee FY, et al. Among authors: menard k. Cancer Chemother Pharmacol. 2009 Jan;63(2):201-12. doi: 10.1007/s00280-008-0727-5. Epub 2008 Mar 19. Cancer Chemother Pharmacol. 2009. PMID: 18350296
62 results