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Synthesis of 14-deoxy-11,12-didehydroandrographolide analogues as potential cytotoxic agents for cholangiocarcinoma |
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| Authors: | Sudarat Sombut Rada Bunthawong Uthaiwan Sirion Teerapich Kasemsuk Pawinee Piyachaturawat Kanoknetr Suksen Apichart Suksamrarn Rungnapha Saeeng |
| Affiliation: | 1. Department of Chemistry and Center for Innovation in Chemistry, Faculty of Science, Burapha University, Chonburi 20131, Thailand;2. Department of Chemistry, Faculty of Science and Technology, Rambhai Barni Rajabhat University, Chanthaburi 22000, Thailand;3. Department of Physiology, Faculty of Science, Mahidol University, Bangkok 10400, Thailand;4. Department of Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok 10240, Thailand |
| Abstract: | A series of 14-deoxy-11,12-didehydroandrographolide analogues were synthesized from naturally occurring andrographolide and their cytotoxicity evaluated against nine cancer cell lines including cholangiocarcinoma. Analogues 5a and 5b exhibited the most potent cytotoxicity with ED50s of 3.37 and 3.08?μM on KKU-M213 cell lines and 2.93 and 3.27?μM on KKU-100 cell lines, respectively. Selective cytotoxicity on cholangiocarcinoma cell lines identified in this study highlight the importance of structural modification in the development of drugs for this cancer. |
| Keywords: | 14-Deoxy-11 12-didehydroandrographolide Cholangiocarcinoma Cytotoxic activity |
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