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

页码：444 / 452

页数：9

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