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Page 1
Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Anderson K, Chen Y, Chen Z, Dominique R, Glenn K, He Y, Janson C, Luk KC, Lukacs C, Polonskaia A, Qiao Q, Railkar A, Rossman P, Sun H, Xiang Q, Vilenchik M, Wovkulich P, Zhang X. Anderson K, et al. Among authors: lukacs c. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. doi: 10.1016/j.bmcl.2013.10.055. Epub 2013 Nov 1. Bioorg Med Chem Lett. 2013. PMID: 24239188
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.
Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC. Liu JJ, et al. Among authors: lukacs c. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. doi: 10.1016/s0960-894x(03)00488-8. Bioorg Med Chem Lett. 2003. PMID: 12852944
Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.
Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM. Liu JJ, et al. Among authors: lukacs c. Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. doi: 10.1016/j.bmcl.2010.08.079. Epub 2010 Aug 21. Bioorg Med Chem Lett. 2010. PMID: 20832307
Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.
Kester RF, Donnell AF, Lou Y, Remiszewski SW, Lombardo LJ, Chen S, Le NT, Lo J, Moliterni JA, Han X, Hogg JH, Liang W, Michoud C, Rupert KC, Mischke S, Le K, Weisel M, Janson CA, Lukacs CM, Fretland AJ, Hong K, Polonskaia A, Gao L, Li S, Solis DS, Aguilar D, Tardell C, Dvorozniak M, Tannu S, Lee EC, Schutt AD, Goggin B. Kester RF, et al. Among authors: lukacs cm. J Med Chem. 2013 Oct 24;56(20):7788-803. doi: 10.1021/jm400732v. Epub 2013 Oct 7. J Med Chem. 2013. PMID: 24093940
Identification of an Adamantyl Azaquinolone JNK Selective Inhibitor.
Haynes NE, Scott NR, Chen LC, Janson CA, Li JK, Lukacs CM, Railkar A, Tozzo E, Whittard T, Brown NF, Cheung AW. Haynes NE, et al. Among authors: lukacs cm. ACS Med Chem Lett. 2012 Aug 8;3(9):764-8. doi: 10.1021/ml300175c. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900545 Free PMC article.
Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.
Donnell AF, Michoud C, Rupert KC, Han X, Aguilar D, Frank KB, Fretland AJ, Gao L, Goggin B, Hogg JH, Hong K, Janson CA, Kester RF, Kong N, Le K, Li S, Liang W, Lombardo LJ, Lou Y, Lukacs CM, Mischke S, Moliterni JA, Polonskaia A, Schutt AD, Solis DS, Specian A, Taylor RT, Weisel M, Remiszewski SW. Donnell AF, et al. Among authors: lukacs cm. J Med Chem. 2013 Oct 24;56(20):7772-87. doi: 10.1021/jm400731m. Epub 2013 Oct 1. J Med Chem. 2013. PMID: 24083782
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Chu XJ, et al. Among authors: lukacs c. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.
Lucas MC, Bhagirath N, Chiao E, Goldstein DM, Hermann JC, Hsu PY, Kirchner S, Kennedy-Smith JJ, Kuglstatter A, Lukacs C, Menke J, Niu L, Padilla F, Peng Y, Polonchuk L, Railkar A, Slade M, Soth M, Xu D, Yadava P, Yee C, Zhou M, Liao C. Lucas MC, et al. Among authors: lukacs c. J Med Chem. 2014 Mar 27;57(6):2683-91. doi: 10.1021/jm401982j. Epub 2014 Feb 26. J Med Chem. 2014. PMID: 24520947
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.
Palmer WS, Alam M, Arzeno HB, Chang KC, Dunn JP, Goldstein DM, Gong L, Goyal B, Hermann JC, Hogg JH, Hsieh G, Jahangir A, Janson C, Jin S, Ursula Kammlott R, Kuglstatter A, Lukacs C, Michoud C, Niu L, Reuter DC, Shao A, Silva T, Trejo-Martin TA, Stein K, Tan YC, Tivitmahaisoon P, Tran P, Wagner P, Weller P, Wu SY. Palmer WS, et al. Among authors: lukacs c. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1486-92. doi: 10.1016/j.bmcl.2012.12.047. Epub 2012 Dec 22. Bioorg Med Chem Lett. 2013. PMID: 23352510
Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.
de Vicente J, Tivitmahaisoon P, Berry P, Bolin DR, Carvajal D, He W, Huang KS, Janson C, Liang L, Lukacs C, Petersen A, Qian H, Yi L, Zhuang Y, Hermann JC. de Vicente J, et al. Among authors: lukacs c. ACS Med Chem Lett. 2015 Aug 4;6(9):1019-24. doi: 10.1021/acsmedchemlett.5b00251. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396691 Free PMC article.
44 results