Anti-HBV and cytotoxic activities of pyranocoumarin derivatives |
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| Authors: | 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 |
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| Affiliation: | 1. Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan;2. Institute of Biochemistry and Molecular Biology, National Yang-Ming University, Taipei 112, Taiwan;3. Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States;4. Division of Medicinal Chemistry and Natural Products, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States |
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| 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 EC50 values of 1.14 and 1.34 μM, 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. |
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