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Molecules 2015, 20(9), 17614-17626; doi:10.3390/molecules200917614

Antibacterial and Antitumor Activities of Biscoumarin and Dihydropyran Derivatives

Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
Beijing Chao-Yang Hospital, Capital Medical University, Beijing 100020, China
Department of Blood Transfusion, Xijing Hospital, the Fourth Military Medical University, Xi’an 710032, China
The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, School of Chemical Engineering, Xi’an University, Xi’an 710065, China
Graduate School of China Academy of Chinese Medical Sciences, Beijing 100700, China
Department of Pharmacology, School of Pharmacy, the Fourth Military Medical University, Xi’an 710032, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 7 August 2015 / Revised: 11 September 2015 / Accepted: 14 September 2015 / Published: 23 September 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [970 KB, uploaded 23 September 2015]   |  


A novel series of biscoumarin (14) and dihydropyran (513) 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 14 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. View Full-Text
Keywords: biscoumarin; dihydropyran; antibacterial; antitumor biscoumarin; dihydropyran; antibacterial; antitumor

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Sui, Y.-P.; Huo, H.-R.; Xin, J.-J.; Li, J.; Li, X.-J.; Du, X.-L.; Ma, H.; Zhou, H.-Y.; Zhan, H.-D.; Wang, Z.-J.; Li, C.; Sui, F.; Li, M.-K. Antibacterial and Antitumor Activities of Biscoumarin and Dihydropyran Derivatives. Molecules 2015, 20, 17614-17626.

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