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Published on: June 26, 2018
Antibacterial and Antitumor Activities of Biscoumarin and Dihydropyran Derivatives
Yun-Peng Sui1,2, Hai-Ru Huo3, Jia-Jia Xin4
1Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China. suiyp8888@sina.com.
Abstract:
A novel series of biscoumarin (1-4) and dihydropyran (5-13) derivatives were synthesized via a one-pot multicomponent condensation reaction and evaluated for antibacterial and antitumor activity in vitro. The X-ray crystal structure analysis of four representative compounds, 3, 7, 9 and 11, confirmed the structures of these compounds. Compounds 1-4 showed the most potent antitumor activity among the total 13 derivatives; especially for compounds 1 and 2, they also emerged as promising antibacterial members with better antibacterial activity. In addition, the results of density functional theory (DFT) showed that compared with compounds 3 and 4, biscoumarins 1 and 2 had lower intramolecular hydrogen bonds (HB) energy in their structures.
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