Abstract
A series of chalcones derivatives were synthesized and evaluated for cytotoxic and antibacterial activities in vitro. These modifications changed their bioactivity profile and indicated a combination of SAR analysis toward the substituents in rings A and B of chalcones. Compounds 2, 6–8, 14–17, and 32 exhibited good cytotoxic properties against two human cancer cell lines HT29 and SGC7901. Compounds 16 and 17 showed high antibacterial activity toward 14 clinically isolated multidrug-resistant strains. Subsequently, the structure of bi-bioactive compound 16 was determined using single-crystal X-ray diffraction. This study presents a few novel leading compounds for the development of potential antitumor and antibacterial agents.
Graphical Abstract
A series of chalcones derivatives were synthesized and evaluated for cytotoxic and antibacterial activities in vitro. Subsequently, the structure of bi-bioactive compound 16 was determined using single-crystal X-ray diffraction.
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Acknowledgments
This study was partially supported by the National Natural Science Funding of China (20802054), Young Talent Funding of Zhejiang Department of Health (2009QN020), Key Project of Wenzhou Sci & Tech Bureau (Y20090009 & Y20100006), and Zhejiang Natural Science Funding (Y2101108 & Y4090261).
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Jianzhang Wu, Cong Wang contribute equally to this work.
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Wu, J., Wang, C., Cai, Y. et al. Synthesis and crystal structure of chalcones as well as on cytotoxicity and antibacterial properties. Med Chem Res 21, 444–452 (2012). https://doi.org/10.1007/s00044-011-9549-9
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DOI: https://doi.org/10.1007/s00044-011-9549-9