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Page 1
Lead optimization toward proof-of-concept tools for Huntington's disease within a 4-(1H-pyrazol-4-yl)pyrimidine class of pan-JNK inhibitors.
Wityak J, McGee KF, Conlon MP, Song RH, Duffy BC, Clayton B, Lynch M, Wang G, Freeman E, Haber J, Kitchen DB, Manning DD, Ismail J, Khmelnitsky Y, Michels P, Webster J, Irigoyen M, Luche M, Hultman M, Bai M, Kuok ID, Newell R, Lamers M, Leonard P, Yates D, Matthews K, Ongeri L, Clifton S, Mead T, Deupree S, Wheelan P, Lyons K, Wilson C, Kiselyov A, Toledo-Sherman L, Beconi M, Muñoz-Sanjuan I, Bard J, Dominguez C. Wityak J, et al. Among authors: kitchen db. J Med Chem. 2015 Apr 9;58(7):2967-87. doi: 10.1021/jm5013598. Epub 2015 Mar 19. J Med Chem. 2015. PMID: 25760409
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties.
Guo C, Hu M, DeOrazio RJ, Usyatinsky A, Fitzpatrick K, Zhang Z, Maeng JH, Kitchen DB, Tom S, Luche M, Khmelnitsky Y, Mhyre AJ, Guzzo PR, Liu S. Guo C, et al. Among authors: kitchen db. Bioorg Med Chem. 2014 Jul 1;22(13):3414-22. doi: 10.1016/j.bmc.2014.04.036. Epub 2014 Apr 28. Bioorg Med Chem. 2014. PMID: 24842618
Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.
Cioffi CL, Dobri N, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Golden KC, Zhu L, Kitchen DB, Barnes KD, Racz B, Qin Q, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. Among authors: kitchen db. J Med Chem. 2014 Sep 25;57(18):7731-57. doi: 10.1021/jm5010013. Epub 2014 Sep 11. J Med Chem. 2014. PMID: 25210858 Free PMC article.
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.
Duffy BC, Liu S, Martin GS, Wang R, Hsia MM, Zhao H, Guo C, Ellis M, Quinn JF, Kharenko OA, Norek K, Gesner EM, Young PR, McLure KG, Wagner GS, Lakshminarasimhan D, White A, Suto RK, Hansen HC, Kitchen DB. Duffy BC, et al. Among authors: kitchen db. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2818-23. doi: 10.1016/j.bmcl.2015.04.107. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 26022843
Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis.
Cioffi CL, Racz B, Varadi A, Freeman EE, Conlon MP, Chen P, Zhu L, Kitchen DB, Barnes KD, Martin WH, Pearson PG, Johnson G, Blaner WS, Petrukhin K. Cioffi CL, et al. Among authors: kitchen db. J Med Chem. 2019 Jun 13;62(11):5470-5500. doi: 10.1021/acs.jmedchem.9b00352. Epub 2019 May 28. J Med Chem. 2019. PMID: 31079449 Free PMC article.
Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.
Cioffi CL, Racz B, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Zhu L, Kitchen DB, Barnes KD, Dobri N, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. Among authors: kitchen db. J Med Chem. 2015 Aug 13;58(15):5863-88. doi: 10.1021/acs.jmedchem.5b00423. Epub 2015 Aug 4. J Med Chem. 2015. PMID: 26181715 Free PMC article.
5-Functionalized indazoles as glucocorticoid receptor agonists.
Bai M, Carr G, Deorazio RJ, Friedrich TD, Dobritsa S, Fitzpatrick K, Guzzo PR, Kitchen DB, Lynch MA, Peace D, Sajad M, Usyatinsky A, Wolf MA. Bai M, et al. Among authors: kitchen db. Bioorg Med Chem Lett. 2010 May 15;20(10):3017-20. doi: 10.1016/j.bmcl.2010.04.012. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20427184
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.
Pechulis AD, Beck JP, Curry MA, Wolf MA, Harms AE, Xi N, Opalka C, Sweet MP, Yang Z, Vellekoop AS, Klos AM, Crocker PJ, Hassler C, Laws M, Kitchen DB, Smith MA, Olson RE, Liu S, Molino BF. Pechulis AD, et al. Among authors: kitchen db. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7219-22. doi: 10.1016/j.bmcl.2012.09.050. Epub 2012 Sep 25. Bioorg Med Chem Lett. 2012. PMID: 23084899
29 results