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Page 1
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
Travins JM, Bernotas RC, Kaufman DH, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J. Travins JM, et al. Among authors: huselton c. Bioorg Med Chem Lett. 2010 Jan 15;20(2):526-30. doi: 10.1016/j.bmcl.2009.11.099. Epub 2009 Nov 23. Bioorg Med Chem Lett. 2010. PMID: 20006495
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
Singhaus RR, Bernotas RC, Steffan R, Matelan E, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J. Singhaus RR, et al. Among authors: huselton c. Bioorg Med Chem Lett. 2010 Jan 15;20(2):521-5. doi: 10.1016/j.bmcl.2009.11.098. Epub 2009 Nov 23. Bioorg Med Chem Lett. 2010. PMID: 20005711
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
Ullrich JW, Morris R, Bernotas RC, Travins JM, Jetter J, Unwalla R, Quinet E, Nambi P, Feingold I, Huselton C, Enroth C, Wilhelmsson A, Goos-Nilsson A, Wrobel J. Ullrich JW, et al. Among authors: huselton c. Bioorg Med Chem Lett. 2010 May 1;20(9):2903-7. doi: 10.1016/j.bmcl.2010.03.031. Epub 2010 Mar 9. Bioorg Med Chem Lett. 2010. PMID: 20382019
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
Hu B, Collini M, Unwalla R, Miller C, Singhaus R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Resmini C, Liu QY, Feingold I, Huselton C, Azam F, Farnegardh M, Enroth C, Bonn T, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J. Hu B, et al. Among authors: huselton c. J Med Chem. 2006 Oct 19;49(21):6151-4. doi: 10.1021/jm0609566. J Med Chem. 2006. PMID: 17034119
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.
Hu B, Jetter J, Kaufman D, Singhaus R, Bernotas R, Unwalla R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Liu QY, Feingold I, Huselton C, Azam F, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J. Hu B, et al. Among authors: huselton c. Bioorg Med Chem. 2007 May 15;15(10):3321-33. doi: 10.1016/j.bmc.2007.03.013. Epub 2007 Mar 12. Bioorg Med Chem. 2007. PMID: 17391964
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Pelletier JC, Chengalvala M, Cottom J, Feingold I, Garrick L, Green D, Hauze D, Huselton C, Jetter J, Kao W, Kopf GS, Lundquist JT 4th, Mann C, Mehlmann J, Rogers J, Shanno L, Wrobel J. Pelletier JC, et al. Among authors: huselton c. Bioorg Med Chem. 2008 Jul 1;16(13):6617-40. doi: 10.1016/j.bmc.2008.05.024. Epub 2008 May 11. Bioorg Med Chem. 2008. PMID: 18511284
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
Wrobel J, Steffan R, Bowen SM, Magolda R, Matelan E, Unwalla R, Basso M, Clerin V, Gardell SJ, Nambi P, Quinet E, Reminick JI, Vlasuk GP, Wang S, Feingold I, Huselton C, Bonn T, Farnegardh M, Hansson T, Nilsson AG, Wilhelmsson A, Zamaratski E, Evans MJ. Wrobel J, et al. Among authors: huselton c. J Med Chem. 2008 Nov 27;51(22):7161-8. doi: 10.1021/jm800799q. J Med Chem. 2008. PMID: 18973288
Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.
Hauze DB, Chengalvala MV, Cottom JE, Feingold IB, Garrick L, Green DM, Huselton C, Kao W, Kees K, Lundquist JT 4th, Mann CW, Mehlmann JF, Rogers JF, Shanno L, Wrobel J, Pelletier JC. Hauze DB, et al. Among authors: huselton c. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1986-90. doi: 10.1016/j.bmcl.2009.02.043. Epub 2009 Feb 13. Bioorg Med Chem Lett. 2009. PMID: 19251413
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Pelletier JC, Chengalvala MV, Cottom JE, Feingold IB, Green DM, Hauze DB, Huselton CA, Jetter JW, Kopf GS, Lundquist JT, Magolda RL, Mann CW, Mehlmann JF, Rogers JF, Shanno LK, Adams WR, Tio CO, Wrobel JE. Pelletier JC, et al. Among authors: huselton ca. J Med Chem. 2009 Apr 9;52(7):2148-52. doi: 10.1021/jm801572m. J Med Chem. 2009. PMID: 19271735
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.
Blass BE, Fensome A, Trybulski E, Magolda R, Gardell SJ, Liu K, Samuel M, Feingold I, Huselton C, Jackson CM, Djandjighian L, Ho D, Hennan J, Janusz JM. Blass BE, et al. Among authors: huselton c. J Med Chem. 2009 Nov 12;52(21):6531-4. doi: 10.1021/jm901042m. J Med Chem. 2009. PMID: 19888755
38 results