Antibacterial and Antitumor Activities of Biscoumarin and Dihydropyran Derivatives

Molecules

Yun-Peng Sui⁴  Hai-Ru Huo⁴  Jia-Jia Xin⁵  Jing Li¹  Xiao-Jun Li¹  Xin-Liang Du²  Hai Ma⁴  Hai-Yu Zhou⁴  Hong-Dan Zhan⁴  Zhu-Ju Wang⁴  Chun Li⁴  Feng Sui⁴  Ming-Kai Li³ 

[1] The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, School of Chemical Engineering, Xi’an University, Xi’an 710065, China; E-Mails:;Graduate School of China Academy of Chinese Medical Sciences, Beijing 100700, China; E-Mail:;Department of Pharmacology, School of Pharmacy, the Fourth Military Medical University, Xi’an 710032, China;Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China; E-Mails:;Department of Blood Transfusion, Xijing Hospital, the Fourth Military Medical University, Xi’an 710032, China; E-Mail:

关键词: biscoumarin;    dihydropyran;    antibacterial;    antitumor;   

DOI  :  10.3390/molecules200917614

来源: mdpi

【 摘 要 】

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.

【 授权许可】

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© 2015 by the authors; licensee MDPI, Basel, Switzerland.