Silica Gel-Mediated Amide Bond Formation: An Environmentally Benign Method for Liquid-Phase Synthesis and Cytotoxic Activities of Amides

被引:36
|
作者
Yang, Xiao-Dong [1 ]
Zeng, Xiang-Hui [1 ]
Zhao, Yuan-Hong [1 ]
Wang, Xue-Quan [1 ]
Pan, Zhi-Qiang [1 ]
Li, Liang [1 ]
Zhang, Hong-Bin [1 ]
机构
[1] Yunnan Univ, Key Lab Med Chem Nat Resource, Minist Educ, Sch Chem Sci & Technol, Kunming 650091, Peoples R China
来源
JOURNAL OF COMBINATORIAL CHEMISTRY | 2010年 / 12卷 / 03期
关键词
PEPTIDE COUPLING REAGENTS; EFFICIENT; COMBINATORIAL; LIBRARIES; IMMONIUM; AMINES;
D O I
10.1021/cc900135f
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
An efficient, functional group tolerable, and environmentally benign process for the synthesis of amides was developed. No activation reagents or scavengers are required in this process. Purification of desired compounds is easy, rapid, and cost-effective. This protocol provides an alternative for the combinatorial liquid-phase synthesis of amide libraries for drug discovery. By this method, a number of amides were prepared and evaluated in vitro against a panel of human tumor cell lines. Cinnamic amide IV-4 was found to be the most potent compound synthesized against four human tumor cell lines. © 2010 American Chemical Society.
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页码:307 / 310
页数:4
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