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ID: ALA1142013

Journal: Bioorg Med Chem Lett

Title: Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.

Authors: Weinstein DS, Liu W, Gu Z, Langevine C, Ngu K, Fadnis L, Combs DW, Sitkoff D, Ahmad S, Zhuang S, Chen X, Wang FL, Loughney DA, Atwal KS, Zahler R, Macor JE, Madsen CS, Murugesan N.

Abstract: 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 inhibitors of the isolated enzyme. Selected compounds also demonstrated desirable inhibition selectivities over isozymes 5- and P-12-LO.

CiteXplore: 15713402

DOI: 10.1016/j.bmcl.2004.12.081