Bioorganic & Medicinal Chemistry Letters 2014-07-01

Synthesis and structure-activity relationship of cyclopentenone oximes as novel inhibitors of the production of tumor necrosis factor-α.

Yeonjoon Kim, Yong Deog Hong, Yung Hyup Joo, Byung Young Woo, Sun-Young Kim, Hyun Ju Koh, Miyoung Park, Kyoung Hee Byoun, Song Seok Shin

Index: Bioorg. Med. Chem. Lett. 24(13) , 2807-10, (2014)

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Abstract

3-Alkyl-2-aryl-2-cyclopenten-1-one oxime derivatives (1) were studied as a novel class of inhibitors of tumor necrosis factor α (TNF-α) with regard to synthesis and in vitro SAR inhibition of TNF-α. The in vitro IC50 values of these compounds in rat and human peripheral blood mononuclear cells were at the sub-micromolar level. Copyright © 2014 Elsevier Ltd. All rights reserved.