Novel natural product-based cinnamates and their thio and thiono analogs as potent inhibitors of cell adhesion molecules on human endothelial cells
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文摘
In the present study, we report the design and synthesis of novel analogs of cinnamates, thiocinnamates and thionocinnamates and evaluated the potencies of these analogs to inhibit TNF-¦Á induced ICAM-1 expression on human endothelial cells. By using whole cell-ELISA, our screening data demonstrated that ethyl 3¡ä,4¡ä,5¡ä-trimethoxythionocinnamate (ETMTC) is the most potent inhibitor of TNF-¦Á induced ICAM-1, VCAM-1 and E-selectin. As functional consequences, ETMTC abrogated TNF-¦Á induced adhesion of neutrophils to the endothelial monolayer. Structure-activity relationship studies revealed the critical role of the chain-length of the alkyl group in the alcohol moiety, number of methoxy groups in the aromatic ring of the cinnamoyl moiety and the presence of the ¦Á, ¦Â- C-C double bond in the thiocinnamates and thionocinnamates.

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