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Page 1
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Lampe JW, Alford JS, Boriak-Sjodin PA, Brach D, Cosmopoulos K, Duncan KW, Eckley ST, Foley MA, Harvey DM, Motwani V, Munchhof MJ, Raimondi A, Riera TV, Tang C, Thomenius MJ, Totman J, Farrow NA. Lampe JW, et al. Among authors: foley ma. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545. doi: 10.1021/acsmedchemlett.1c00272. eCollection 2021 Oct 14. ACS Med Chem Lett. 2021. PMID: 34671445 Free PMC article.
Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.
Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R. Mitchell LH, et al. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985287 Free PMC article.
Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA. Thomenius MJ, et al. PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018. PLoS One. 2018. PMID: 29856759 Free PMC article.
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
Lee KL, Foley MA, Chen L, Behnke ML, Lovering FE, Kirincich SJ, Wang W, Shim J, Tam S, Shen MW, Khor S, Xu X, Goodwin DG, Ramarao MK, Nickerson-Nutter C, Donahue F, Ku MS, Clark JD, McKew JC. Lee KL, et al. Among authors: foley ma. J Med Chem. 2007 Mar 22;50(6):1380-400. doi: 10.1021/jm061131z. Epub 2007 Feb 17. J Med Chem. 2007. PMID: 17305324
Inhibition of cytosolic phospholipase A2alpha: hit to lead optimization.
McKew JC, Foley MA, Thakker P, Behnke ML, Lovering FE, Sum FW, Tam S, Wu K, Shen MW, Zhang W, Gonzalez M, Liu S, Mahadevan A, Sard H, Khor SP, Clark JD. McKew JC, et al. Among authors: foley ma. J Med Chem. 2006 Jan 12;49(1):135-58. doi: 10.1021/jm0507882. J Med Chem. 2006. PMID: 16392799
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. Among authors: foley ma. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC. Lee KL, et al. Among authors: foley ma. Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. doi: 10.1016/j.bmc.2007.10.060. Epub 2007 Oct 22. Bioorg Med Chem. 2008. PMID: 17998165
97 results