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Synthesis and cytotoxic activity of 14-deoxy-12-hydroxyandrographolide analogs

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Abstract

Important anticancer cytotoxicological properties are reported from synthetic analogs of 14-deoxy-12-hydroxy-andrographolide, a compound that occurs in Andrographis paniculata, an indigenous Southeast Asia plant. Cytotoxicities of 15 synthesized 14-deoxy-12-hydroxy-andrographolide analogs were evaluated against a panel of cancer cell lines with some exhibiting much greater than the parent compound. For example analog 2j was 6–35 times more potent than the parent compound and the anticancer agent, ellipticin, on all cell lines except LU-1 cancer cells. With promising cytotoxicities and simple preparation, this compound has significant potential in the treatment of cancer.

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Acknowledgements

This work was supported by Research Grant of Burapha University through National Research Council of Thailand (39/2557) and the Center of Excellence for Innovation in Chemistry (PERCH-CIC). Partial support from the Strategic Basic Research Grant of The Thailand Research Fund to R.S. (DBG5680004) and A.S. (DBG5980003) are gratefully acknowledged. Special thanks to Prof. Dr Frederick W. H. Beamish, Faculty of Science, Burapha University, for his comments and English correction.

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Correspondence to Rungnapha Saeeng.

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Sirion, U., Kasemsuk, T., Piyachaturawat, P. et al. Synthesis and cytotoxic activity of 14-deoxy-12-hydroxyandrographolide analogs. Med Chem Res 26, 1653–1663 (2017). https://doi.org/10.1007/s00044-017-1881-2

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  • DOI: https://doi.org/10.1007/s00044-017-1881-2

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