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Abstract Title:

Anti-HBV and cytotoxic activities of pyranocoumarin derivatives.

Abstract Source:

Bioorg Med Chem. 2009 Aug 15;17(16):6137-43. Epub 2008 Dec 13. PMID: 19635670

Abstract Author(s):

Chung-Ren Su, Sheau Farn Yeh, Chih Miem Liu, Amooru G Damu, Tsung-Hsiao Kuo, Po-Cheng Chiang, Kenneth F Bastow, Kuo-Hsiung Lee, Tian-Shung Wu

Article Affiliation:

Department of Chemistry, National Cheng Kung University, Tainan, Taiwan.

Abstract:

Four natural pyranocoumarins clausenidin (1), nordentatin (2), clausarin (3), and xanthoxyletin (4) were isolated from the medicinal plant Clausena excavata. Recently, we found that 1 and 2 suppressed hepatitis B virus surface antigen in HepA2 cells, and in addition, 1-3 showed cytotoxic activity against four human cancer cell lines (A549, MCF7, KB, and KB-VIN). To explore the SAR of 1-4, 17 pyranocoumarin analogues (5-21) were designed and synthesized. Among these analogues, 5 and 10 were the most potent against hepatitis B virus with EC(50) values of 1.14 and 1.34microM, respectively. The most interesting result in the cytotoxicity assay was the significant activity of 1, 5, and 6 against the multi-drug resistant cell line, KB-VIN, without activity against the KB cell line. These data suggest that these three compounds could be useful hits for developing MDR-inverse drugs.

Study Type : In Vitro Study

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Sayer Ji
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Depression: 21st Century Solutions + The Dark Side of Wheat

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