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Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities |
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| Authors: | Xiao Qicai Liu Yongqiang Qiu Yatao Yao Zhiyi Zhou Guangbiao Yao Zhu-Jun Jiang Sheng |
| Institution: | a Laboratory of Regenerative Biology, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China b Shanghai Institute of Technology, Shanghai 210032, China c Division of Molecular Carcinogenesis and Targeted Therapy for Cancer, State Key Laboratory of Biomembrane and Membrane Biotechnology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China d State Key Laboratory of Coordination Chemistry, Nanjing National Laboratory of Microstructures, School of Chemistry and Chemical Engineering, Nanjing University, 22 Hankou Road, Nanjing 210093, China |
| Abstract: | A new series of linear dimeric compounds mimicking naturally occurring annonaceous acetogenins have been synthesized by bivalent analogue design, and their cytotoxicities have been evaluated against the growth of cancer cells by MTT method. Most of these compounds show selective action favored to human cancer cell lines over normal cell lines, and compound 9 with bis-terminal benzoquinone functionality exhibits an IC50 = 0.40 μM against MCF7 cell lines. This work mentions that appropriate conformational constraints might be a useful optimizing tool for this unique class of anticancer compounds. |
| Keywords: | Annonaceous acetogenins Mimicry Bivalent analogue Cytotoxicity Selectivity |
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