2. Academic Validation
  3. Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines

Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines

  • Bioorg Med Chem Lett. 2008 Dec 15;18(24):6553-7. doi: 10.1016/j.bmcl.2008.10.046.
Chun-nian Xia 1,  Hai-bo Li,  Feng Liu,  Wei-xiao Hu
Affiliations

Affiliation

  • 1 College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032, PR China.
PMID: 18952420 DOI: 10.1016/j.bmcl.2008.10.046
Abstract

Forty caffeate analogues were synthesized via a convenient method starting from vanillin with moderate to good yields. The testing of biological activity of these compounds against HIV-1 integrase indicates that four compounds: bornyl caffeate, bornyl 2-nitrocaffeate, 5-nitrocaffeic acid and 5-nitrocaffeic acid phenethyl ester (5-nitroCAPE) possess a good HIV Integrase inhibitory activity, IC(50) 19.9, 26.8, 25.0 and 13.5 microM , respectively. Twelve caffeate analogues were tested by MTT assay on growth of human hepatocellular carcinoma BEL-7404, human breast MCF-7 adenocarcinoma, human lung A549 adenocarcinoma and human gastric Cancer BCG823 cell lines, respectively. And the best result is IC(50) 5.5 microM for CAPE against BEL-7404.

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