The Synthesis and Biological Evaluation of Aloe-Emodin-Coumarin Hybrids as Potential Antitumor Agents |
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| Authors: | Hai Shang Yue Hu Jingrong Li Lingyu Li Yu Tian Xiaoxue Li Qi Wu Zhongmei Zou |
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| Affiliation: | 1.Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China;2.School of Basic Medical Sciences, Guizhou Medical University, Guiyang 550025, China;3.School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China;4.School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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| Abstract: | A series of novel aloe-emodin–coumarin hybrids were designed and synthesized. The antitumor activity of these derivatives was evaluated against five human tumor cell lines (A549, SGC-7901, HepG2, MCF-7 and HCT-8). Some of the synthesized compounds exhibited moderate to good activity against one or more cell lines. Particularly, compound 5d exhibited more potent antiproliferative activity than the reference drug etoposide against all tested tumor cell lines, indicating that it had a broad spectrum of antitumor activity and that it may provide a promising lead compound for further development as an antitumor agent by structural modification. Furthermore, the structure–activity relationship study of the synthesized compounds was also performed. |
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| Keywords: | aloe-emodin coumarin hybrid structural modification antitumor activity |
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