| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374807 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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, IC50 19.9, 26.8, 25.0 and 13.5 μM, 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 IC50 5.5 μM for CAPE against BEL-7404.
Graphical abstractForty caffeate analogues synthesized by one-pot methods were evaluated for their bioactivities. Four caffeate analogues possessed good HIV-IN inhibitory activities and several compounds showed good antitumor activities.Figure optionsDownload full-size imageDownload as PowerPoint slide
