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Fused tricyclic indoles as S1P₁ agonists with robust efficacy in animal models of autoimmune disease
Autor:
Daniel J, Buzard, Sangdon, Han, Luis, Lopez, Andrew, Kawasaki, Jeanne, Moody, Lars, Thoresen, Brett, Ullman, Juerg, Lehmann, Imelda, Calderon, Xiuwen, Zhu, Tawfik, Gharbaoui, Dipanjan, Sengupta, Ashwin, Krishnan, Yinghong, Gao, Jeff, Edwards, Jeremy, Barden, Michael, Morgan, Khawja, Usmani, Chuan, Chen, Abu, Sadeque, Jayant, Thatte, Michelle, Solomon, Lixia, Fu, Kevin, Whelan, Ling, Liu, Hussien, Al-Shamma, Joel, Gatlin, Minh, Le, Charles, Xing, Sheryll, Espinola, Robert M, Jones
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(13)
Two series of fused tricyclic indoles were identified as potent and selective S1P(1) agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoim