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Page 1
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV. Zimmermann K, et al. Among authors: mastalerz ha. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 25987372
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV. Harikrishnan LS, et al. Among authors: mastalerz ha. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21282055
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. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Fink BE, Vite GD, Mastalerz H, Kadow JF, Kim SH, Leavitt KJ, Du K, Crews D, Mitt T, Wong TW, Hunt JT, Vyas DM, Tokarski JS. Fink BE, et al. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4774-9. doi: 10.1016/j.bmcl.2005.07.027. Bioorg Med Chem Lett. 2005. PMID: 16111887
The discovery of BMS-275183: an orally efficacious novel taxane.
Mastalerz H, Cook D, Fairchild CR, Hansel S, Johnson W, Kadow JF, Long BH, Rose WC, Tarrant J, Wu MJ, Xue MQ, Zhang G, Zoeckler M, Vyas DM. Mastalerz H, et al. Bioorg Med Chem. 2003 Oct 1;11(20):4315-23. doi: 10.1016/s0968-0896(03)00495-4. Bioorg Med Chem. 2003. PMID: 13129567
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Dextraze P, Fink BE, Gavai A, Goyal B, Han WC, Johnson W, Langley D, Lee FY, Marathe P, Mathur A, Oppenheimer S, Ruediger E, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2036-42. doi: 10.1016/j.bmcl.2007.01.002. Epub 2007 Jan 12. Bioorg Med Chem Lett. 2007. PMID: 17270437
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Fink BE, Gavai A, Han WC, Johnson W, Langley D, Lee FY, Leavitt K, Marathe P, Norris D, Oppenheimer S, Sleczka B, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4947-54. doi: 10.1016/j.bmcl.2007.06.019. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17606372
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC, Norris D, Goyal B, Swaminathan S, Patel B, Mathur A, Vyas DM, Tokarski JS, Yu C, Oppenheimer S, Zhang H, Marathe P, Fargnoli J, Lee FY, Wong TW, Vite GD. Gavai AV, et al. J Med Chem. 2009 Nov 12;52(21):6527-30. doi: 10.1021/jm9010065. J Med Chem. 2009. PMID: 19821562
18 results