Synthesis and evaluation of novel substituted 5-hydroxycoumarin and pyranocoumarin derivatives exhibiting significant antiproliferative activity against breast cancer cell lines |
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Authors: | Wei-wei Mao Ting-ting Wang He-ping Zeng Zhi-yu Wang Jian-ping Chen Jian-gang Shen |
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Affiliation: | 1. Institute of Functional Molecule, South China University of Technology, Guangzhou 510641, People’s Republic of China;2. School of Chemistry and Environment, South China Normal University, Guangzhou 510631, People’s Republic of China;3. School of Chinese Medicine, The University of Hong Kong, 10 Sassoon Road, Hong Kong, People’s Republic of China |
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Abstract: | A library of novel 5-hydroxycoumarin and pyranocoumarin derivatives was constructed via silica sulfuric acid-catalyzed pechmann reaction and Pd(0)-catalyzed suzuki coupling in tandem, and their antiproliferative activities against breast cancer cells MCF-7 and MDA-MB-231 were evaluated. The results showed that compounds such as 6b, 6d, 6h, and 6k possess significant antiproliferative activity against MCF-7 cell line with the IC50 values of 7.2, 5.3, 3.3, and 6.5 μM, respectively. |
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