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Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
Laufer R, Ng G, Liu Y, Patel NK, Edwards LG, Lang Y, Li SW, Feher M, Awrey DE, Leung G, Beletskaya I, Plotnikova O, Mason JM, Hodgson R, Wei X, Mao G, Luo X, Huang P, Green E, Kiarash R, Lin DC, Harris-Brandts M, Ban F, Nadeem V, Mak TW, Pan GJ, Qiu W, Chirgadze NY, Pauls HW. Laufer R, et al. Among authors: chirgadze ny. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97. doi: 10.1016/j.bmc.2014.06.027. Epub 2014 Jun 23. Bioorg Med Chem. 2014. PMID: 25043312
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.
Liu Y, Lang Y, Patel NK, Ng G, Laufer R, Li SW, Edwards L, Forrest B, Sampson PB, Feher M, Ban F, Awrey DE, Beletskaya I, Mao G, Hodgson R, Plotnikova O, Qiu W, Chirgadze NY, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW. Liu Y, et al. Among authors: chirgadze ny. J Med Chem. 2015 Apr 23;58(8):3366-92. doi: 10.1021/jm501740a. Epub 2015 Apr 3. J Med Chem. 2015. PMID: 25763473
Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.
Liu Y, Laufer R, Patel NK, Ng G, Sampson PB, Li SW, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Plotnikova O, Awrey DE, Qiu W, Chirgadze NY, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Fletcher GC, Mak TW, Bray MR, Pauls HW. Liu Y, et al. Among authors: chirgadze ny. ACS Med Chem Lett. 2016 May 6;7(7):671-5. doi: 10.1021/acsmedchemlett.5b00485. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437075 Free PMC article.
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
Sampson PB, Liu Y, Patel NK, Feher M, Forrest B, Li SW, Edwards L, Laufer R, Lang Y, Ban F, Awrey DE, Mao G, Plotnikova O, Leung G, Hodgson R, Mason JM, Wei X, Kiarash R, Green E, Qiu W, Chirgadze NY, Mak TW, Pan G, Pauls HW. Sampson PB, et al. Among authors: chirgadze ny. J Med Chem. 2015 Jan 8;58(1):130-46. doi: 10.1021/jm5005336. Epub 2014 Jun 24. J Med Chem. 2015. PMID: 24867403
Insights into the binding of PARP inhibitors to the catalytic domain of human tankyrase-2.
Qiu W, Lam R, Voytyuk O, Romanov V, Gordon R, Gebremeskel S, Vodsedalek J, Thompson C, Beletskaya I, Battaile KP, Pai EF, Rottapel R, Chirgadze NY. Qiu W, et al. Among authors: chirgadze ny. Acta Crystallogr D Biol Crystallogr. 2014 Oct;70(Pt 10):2740-53. doi: 10.1107/S1399004714017660. Epub 2014 Sep 27. Acta Crystallogr D Biol Crystallogr. 2014. PMID: 25286857 Free PMC article.
Crystal structure of the CN-hydrolase SA0302 from the pathogenic bacterium Staphylococcus aureus belonging to the Nit and NitFhit Branch of the nitrilase superfamily.
Gordon RD, Qiu W, Romanov V, Lam K, Soloveychik M, Benetteraj D, Battaile KP, Chirgadze YN, Pai EF, Chirgadze NY. Gordon RD, et al. Among authors: chirgadze ny, chirgadze yn. J Biomol Struct Dyn. 2013 Oct;31(10):1057-65. doi: 10.1080/07391102.2012.719111. Epub 2012 Oct 2. J Biomol Struct Dyn. 2013. PMID: 23607706
Structure of Francisella tularensis peptidyl-tRNA hydrolase.
Clarke TE, Romanov V, Lam R, Gothe SA, Peddi SR, Razumova EB, Lipman RS, Branstrom AA, Chirgadze NY. Clarke TE, et al. Among authors: chirgadze ny. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2011 Apr 1;67(Pt 4):446-9. doi: 10.1107/S174430911100515X. Epub 2011 Mar 26. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2011. PMID: 21505237 Free PMC article.
43 results