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Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Li JJ, Iula DM, Nguyen MN, Hu LY, Dettling D, Johnson TR, Du DY, Shanmugasundaram V, Van Camp JA, Wang Z, Harter WG, Yue WS, Boys ML, Wade KJ, Drummond EM, Samas BM, Lefker BA, Hoge GS, Lovdahl MJ, Asbill J, Carroll M, Meade MA, Ciotti SM, Krieger-Burke T. Li JJ, et al. Among authors: lefker ba. J Med Chem. 2008 Nov 13;51(21):7010-4. doi: 10.1021/jm8009316. Epub 2008 Oct 16. J Med Chem. 2008. PMID: 18921992
(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.
Hu LY, Du D, Hoffman J, Smith Y, Fedij V, Kostlan C, Johnson TR, Huang Y, Kesten S, Harter W, Yue WS, Li JJ, Barvian N, Mitchell L, Lei HJ, Lefker B, Carroll M, Dettling D, Krieger-Burke T, Samas B, Yalamanchili R, Lapham K, Pocalyko D, Sliskovic D, Ciotti S, Stoller B, Hena MA, Ding Q, Maiti SN, Stier M, Welgus H. Hu LY, et al. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5983-8. doi: 10.1016/j.bmcl.2007.07.075. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17827000
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P. Chesworth R, et al. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. doi: 10.1016/j.bmcl.2005.08.010. Epub 2005 Oct 10. Bioorg Med Chem Lett. 2005. PMID: 16219463
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
McClure KF, Darout E, Guimarães CR, DeNinno MP, Mascitti V, Munchhof MJ, Robinson RP, Kohrt J, Harris AR, Moore DE, Li B, Samp L, Lefker BA, Futatsugi K, Kung D, Bonin PD, Cornelius P, Wang R, Salter E, Hornby S, Kalgutkar AS, Chen Y. McClure KF, et al. Among authors: lefker ba. J Med Chem. 2011 Mar 24;54(6):1948-52. doi: 10.1021/jm200003p. Epub 2011 Mar 1. J Med Chem. 2011. PMID: 21361292
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.
Liang SH, Chen JM, Normandin MD, Chang JS, Chang GC, Taylor CK, Trapa P, Plummer MS, Para KS, Conn EL, Lopresti-Morrow L, Lanyon LF, Cook JM, Richter KE, Nolan CE, Schachter JB, Janat F, Che Y, Shanmugasundaram V, Lefker BA, Enerson BE, Livni E, Wang L, Guehl NJ, Patnaik D, Wagner FF, Perlis R, Holson EB, Haggarty SJ, El Fakhri G, Kurumbail RG, Vasdev N. Liang SH, et al. Among authors: lefker ba. Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5. doi: 10.1002/anie.201603797. Epub 2016 Jun 29. Angew Chem Int Ed Engl. 2016. PMID: 27355874 Free PMC article.
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
Chesworth R, Zawistoski MP, Lefker BA, Cameron KO, Day RF, Mangano FM, Rosati RL, Colella S, Petersen DN, Brault A, Lu B, Pan LC, Perry P, Ng O, Castleberry TA, Owen TA, Brown TA, Thompson DD, DaSilva-Jardine P. Chesworth R, et al. Among authors: lefker ba. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2729-33. doi: 10.1016/j.bmcl.2004.03.077. Bioorg Med Chem Lett. 2004. PMID: 15125923
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Mascitti V, Stevens BD, Choi C, McClure KF, Guimarães CR, Farley KA, Munchhof MJ, Robinson RP, Futatsugi K, Lavergne SY, Lefker BA, Cornelius P, Bonin PD, Kalgutkar AS, Sharma R, Chen Y. Mascitti V, et al. Among authors: lefker ba. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9. doi: 10.1016/j.bmcl.2011.01.088. Epub 2011 Jan 25. Bioorg Med Chem Lett. 2011. PMID: 21310611
37 results