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
  • 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.