Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.

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Yao RS, Lu XQ, Guan QX, Zheng L, Lu X, Ruan BF

Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.

Eur J Med Chem. 2013 Apr;62:222-31. doi: 10.1016/j.ejmech.2012.11.021. Epub 2012 Nov 20.

PubMed ID

23353741 [ View in PubMed

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Abstract

Three series of novel resveratrol amide derivatives (1a-q, 2a-h, 3a-l) were synthesized and evaluated for their biological activities. All compounds were characterized by (1)H NMR, (13)C NMR, MS and elemental analysis. Furthermore, compound 3e was also characterized by X-ray crystallography. All the compounds were evaluated for their anti-tumor activity against MCF-7, A549 and B16-F10 tumor cell lines as well as cyclooxygenase-2 (COX-2)-derived prostaglandin E2 (PGE2) inhibitory activity of murine macrophage RAW 264.7 cell line. Among them, compounds 1c, 1g and 3e displayed the most potent COX-2 inhibitory activity with the IC50 values of 1.02, 1.27 and 1.98 muM, respectively. Molecular docking studies were performed to position compounds 1c and 3e into the active site of COX-2 to determine the probable binding modes.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Celecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	100	N/A	N/A	Details