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

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.

journal_name

Bioorg Med Chem Lett

authors

Xia CN,Li HB,Liu F,Hu WX

doi

10.1016/j.bmcl.2008.10.046

subject

Has Abstract

pub_date

2008-12-15 00:00:00

pages

6553-7

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01247-X

journal_volume

18

pub_type

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