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Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r. J Med Chem. 2010. PMID: 20184326
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
Ali A, Thompson CF, Balkovec JM, Graham DW, Hammond ML, Quraishi N, Tata JR, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Thompson CM, Zaller DM, Forrest MJ, Carballo-Jane E, Luell S. Ali A, et al. J Med Chem. 2004 May 6;47(10):2441-52. doi: 10.1021/jm030585i. J Med Chem. 2004. PMID: 15115388
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S. Thompson CF, et al. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7. doi: 10.1016/j.bmcl.2005.02.009. Bioorg Med Chem Lett. 2005. PMID: 15808489
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.
Smith CJ, Ali A, Balkovec JM, Graham DW, Hammond ML, Patel GF, Rouen GP, Smith SK, Tata JR, Einstein M, Ge L, Harris GS, Kelly TM, Mazur P, Thompson CM, Wang CF, Williamson JM, Miller DK, Pandit S, Santoro JC, Sitlani A, Yamin TT, O'Neill EA, Zaller DM, Carballo-Jane E, Forrest MJ, Luell S. Smith CJ, et al. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2926-31. doi: 10.1016/j.bmcl.2005.03.027. Bioorg Med Chem Lett. 2005. PMID: 15911283
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.
Thompson CF, Quraishi N, Ali A, Mosley RT, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S. Thompson CF, et al. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3354-61. doi: 10.1016/j.bmcl.2007.03.103. Epub 2007 Apr 5. Bioorg Med Chem Lett. 2007. PMID: 17467988
41 results