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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: zhang g. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
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. Among authors: zhang g. Bioorg Med Chem. 2003 Oct 1;11(20):4315-23. doi: 10.1016/s0968-0896(03)00495-4. Bioorg Med Chem. 2003. PMID: 13129567
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Gavai A, Johnson W, Langley D, Lee FY, Marathe P, Mathur A, Oppenheimer S, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G. Mastalerz H, et al. Among authors: zhang g, zhang h. Bioorg Med Chem Lett. 2007 May 15;17(10):2828-33. doi: 10.1016/j.bmcl.2007.02.050. Epub 2007 Feb 27. Bioorg Med Chem Lett. 2007. PMID: 17368025
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: zhang g. 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
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: zhang g. 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
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. Among authors: zhang g, zhang h. 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. Among authors: zhang g, zhang h. 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
The structure of human tau-tubulin kinase 1 both in the apo form and in complex with an inhibitor.
Kiefer SE, Chang CJ, Kimura SR, Gao M, Xie D, Zhang Y, Zhang G, Gill MB, Mastalerz H, Thompson LA, Cacace AM, Sheriff S. Kiefer SE, et al. Among authors: zhang g, zhang y. Acta Crystallogr F Struct Biol Commun. 2014 Feb;70(Pt 2):173-81. doi: 10.1107/S2053230X14000144. Epub 2014 Jan 21. Acta Crystallogr F Struct Biol Commun. 2014. PMID: 24637750 Free PMC article.
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