862115-66-0Relevant academic research and scientific papers
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase
Weinstein, David S.,Liu, Wen,Gu, Zhengxiang,Langevine, Charles,Ngu, Khehyong,Fadnis, Leena,Combs, Donald W.,Sitkoff, Doree,Ahmad, Saleem,Zhuang, Shaobin,Chen, Xing,Wang, Feng-Lai,Loughney, Deborah A.,Atwal, Karnail S.,Zahler, Robert,Macor, John E.,Madsen, Cort S.,Murugesan, Natesan
, p. 1435 - 1440 (2007/10/03)
A series of inhibitors of mammalian 15-lipoxygenase based on tryptamine and homotryptamine scaffolds is described. Compounds with aryl substituents at C-2 of the indole core of tryptamine and homotryptamine sulfonamides (e.g., 37a-p) proved to be potent i
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles
Chu, Lin,Hutchins, Jennifer E.,Weber, Ann E.,Lo, Jane-Ling,Yang, Yi-Tien,Cheng, Kang,Smith, Roy G.,Fisher, Michael H.,Wyvratt, Matthew J.,Goulet, Mark T.
, p. 509 - 513 (2007/10/03)
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
