Synthesis of licochalcone analogues with increased anti-inflammatory activity

  • Bioorg Med Chem Lett. 2014 Jan 1;24(1):181-5. doi: 10.1016/j.bmcl.2013.11.044.
Si-Jun Kim  1 ,  Cheol Gi Kim  1 ,  So-Ra Yun  1 ,  Jin-Kyung Kim  2 ,  Jong-Gab Jun  3
Affiliations
  • 1. Department of Chemistry and Institute of Applied Chemistry, Hallym University, Chuncheon 200-702, Republic of Korea.
  • 2. Department of Biomedical Science, College of Natural Science, Catholic University of Daegu, Gyeungsan-Si 700-702, Republic of Korea.
  • 3. Department of Chemistry and Institute of Applied Chemistry, Hallym University, Chuncheon 200-702, Republic of Korea. Electronic address: [email protected].
PMID: 24316124 DOI: 10.1016/j.bmcl.2013.11.044
Abstract

Licohalcones have been reported to have various biological activities. However, most of licochalcones also showed cytotoxicity even though their versitile utilities. Licochalcones B and D, which have common substituents at aromatic ring B, are targeted to modify the structure at aromatic ring A for inflammatory studies. Licochalcone derivatives (1-6) thus prepared are compared for their suppression ability of nitric oxide (NO) production and showed 9.94, 4.72, 10.1, 4.85, 2.37 and 4.95μM of IC50 values, respectively.

Keywords
IC(50) values of NO production; Licohalcone B; Licohalcone D; [3,3]-Sigmatropic rearrangement; anti-Inflammatory effects.