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2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV. Harris CM, et al. Among authors: frank ke. Bioorg Med Chem Lett. 2010 Jan 1;20(1):334-7. doi: 10.1016/j.bmcl.2009.10.103. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2010. PMID: 19926477
Design and synthesis of tricyclic cores for kinase inhibition.
Van Epps S, Fiamengo B, Edmunds J, Ericsson A, Frank K, Friedman M, George D, George J, Goedken E, Kotecki B, Martinez G, Merta P, Morytko M, Shekhar S, Skinner B, Stewart K, Voss J, Wallace G, Wang L, Wang L, Wishart N. Van Epps S, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):693-8. doi: 10.1016/j.bmcl.2012.11.108. Epub 2012 Dec 5. Bioorg Med Chem Lett. 2013. PMID: 23265875
Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.
Goedken ER, Argiriadi MA, Banach DL, Fiamengo BA, Foley SE, Frank KE, George JS, Harris CM, Hobson AD, Ihle DC, Marcotte D, Merta PJ, Michalak ME, Murdock SE, Tomlinson MJ, Voss JW. Goedken ER, et al. Among authors: frank ke. J Biol Chem. 2015 Feb 20;290(8):4573-4589. doi: 10.1074/jbc.M114.595181. Epub 2014 Dec 31. J Biol Chem. 2015. PMID: 25552479 Free PMC article.
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.
Friedman M, Frank KE, Aguirre A, Argiriadi MA, Davis H, Edmunds JJ, George DM, George JS, Goedken E, Fiamengo B, Hyland D, Li B, Murtaza A, Morytko M, Somal G, Stewart K, Tarcsa E, Van Epps S, Voss J, Wang L, Woller K, Wishart N. Friedman M, et al. Among authors: frank ke. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4399-404. doi: 10.1016/j.bmcl.2015.09.020. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26372653
Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds.
Ramos AL, Goedken ER, Frank KE, Argiriadi MA, Bazzaz S, Bian Z, Brown JTC, Centrella PA, Chen HJ, Disch JS, Donner PL, Duignan DB, Gikunju D, Greszler SN, Guié MA, Habeshian S, Hartl HE, Hein CD, Hutchins CW, Jetson R, Keefe AD, Khan H, Li HQ, Olszewski A, Ortiz Cardona BJ, Osuma A, Panchal SC, Phelan R, Qiu W, Shotwell JB, Shrestha A, Srikumaran M, Su Z, Sun C, Upadhyay AK, Wood MD, Wu H, Zhang R, Zhang Y, Zhao G, Zhu H, Webster MP. Ramos AL, et al. Among authors: frank ke. J Med Chem. 2024 Apr 25;67(8):6456-6494. doi: 10.1021/acs.jmedchem.3c02397. Epub 2024 Apr 4. J Med Chem. 2024. PMID: 38574366
A simple, inexpensive apparatus for performance of preparative scale solution phase multiple parallel synthesis of drug analogs. II. Biological evaluation of a retrospective library of quinolone antiinfective agents.
Frank KE, Devasthale PV, Gentry EJ, Ravikumar VT, Keschavarz-Shokri A, Mitscher LA, Nilius A, Shen LL, Shawar R, Baker WR. Frank KE, et al. Comb Chem High Throughput Screen. 1998 Jun;1(2):89-99. Comb Chem High Throughput Screen. 1998. PMID: 10500768
32 results