| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375271 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
A series of caffeic acid amide derivatives 2-cyano-(3-substituted phenyl)acrylamides were synthesized via Knoevenogal condensation of substituted benzaldehydes with cyanoacetamides. The structure of compound 1f was determined as E-isomer by X-ray diffractive analysis. The biological screening tests in vitro showed that compound 1b has obvious inhibitory activities against human gastric carcinoma cell line BGC-823, human nasopharyngeal carcinoma cell line KB and human hepatoma cell line BEL-7402 with IC50 values of 5.6 μg/mL, 13.1 μg/mL and 12.5 μg/mL, respectively. Some preliminary structure–activity relationships (SAR) were also proposed which may provide a direction for further study.
Graphical abstractA series of caffeic acid amide derivatives E-2-cyano-(3-substituted phenyl)acrylamides were synthesized via Knoevenogal condensation. Some preliminary structure–activity relationships are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
