Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 23, Pages 5139-5143Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.10.063
Keywords
14-Deoxy-11; 12-didehydroandrographolide; Andrographis paniculata Nees; Cholangiocarcinoma; Cytotoxic activity
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Funding
- Strategic Basic Research Grant of The Thailand Research Fund [DBG5680004]
- Research Grant of Burapha University through National Research Council of Thailand
- Center of Excellence for Innovation in Chemistry (PERCH-CIC)
- Research Grant of The Thailand Research Fund [DBG5980003]
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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 ED(50)s of 3.37 and 3.08 mu M on KKU-M213 cell lines and 2.93 and 3.27 mu M 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. (C) 2017 Elsevier Ltd. All rights reserved.
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