Synthesis and crystal structure of chalcones as well as on cytotoxicity and antibacterial properties

被引：29
作者：
Wu, Jianzhang [1 ,2 ]
Wang, Cong [1 ,3 ]
Cai, Yuepiao [1 ]
Peng, Jing [1 ]
Liang, Donglou [1 ]
Zhao, Yunjie [1 ]
Yang, Shulin [2 ]
Li, Xiaokun [1 ,2 ]
Wu, Xiaoping [1 ,3 ]
Liang, Guang [1 ,2 ]
机构：
[1] Wenzhou Med Coll, Sch Pharm, Bioorgan & Med Chem Res Ctr, Wenzhou 325035, Zhejiang, Peoples R China
[2] Nanjing Univ Sci & Technol, Inst Biotechnol, Nanjing 210094, Jiangsu, Peoples R China
[3] Jinan Univ, Inst Tissue Transplantat & Immunol, Guangzhou 510632, Guangdong, Peoples R China
来源：
MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 04期
关键词：
Chalcones; Synthesis; Cytotoxicity; Antibacterial activity; Crystal structure; IN-VITRO; DERIVATIVES; MACROPHAGES; INDUCTION; ANALOGS; DESIGN; AGENTS;
D O I：
10.1007/s00044-011-9549-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：444 / 452
页数：9
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