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

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

  • Bioorg Med Chem Lett. 2014 Jul 1;24(13):2807-10. doi: 10.1016/j.bmcl.2014.04.115.
Yeonjoon Kim 1,  Yong Deog Hong 2,  Yung Hyup Joo 3,  Byung Young Woo 3,  Sun-Young Kim 3,  Hyun Ju Koh 3,  Miyoung Park 3,  Kyoung Hee Byoun 3,  Song Seok Shin 4
Affiliations

Affiliations

  • 1 AmorePacific R&D Unit, 314-1 Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do 449-729, Republic of Korea; Solvay Korea, Ewha-Solvay R&I Center 150, Bukahyun-ro, Seodaemun-gu, Seoul, Republic of Korea.
  • 2 AmorePacific R&D Unit, 314-1 Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do 449-729, Republic of Korea. Electronic address: [email protected].
  • 3 AmorePacific R&D Unit, 314-1 Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do 449-729, Republic of Korea.
  • 4 AmorePacific R&D Unit, 314-1 Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do 449-729, Republic of Korea. Electronic address: [email protected].
PMID: 24852119 DOI: 10.1016/j.bmcl.2014.04.115
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.

Keywords

Cyclopentenone oximes; PBMCs; SAR; TNF-α.

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