Synthesis and Evaluation of Some 17-Acetamidoandrostane and N,N-Dimethyl-7-deoxycholic Amide Derivatives as Cytotoxic Agents: Structure/Activity Studies

Molecules

Yanmin Huang³  Jianguo Cui³  Linyi Jia¹  Chunfang Gan³  Huacan Song²  Chun Zeng⁴ 

[1] No. 37 Middel School in Nanning, Nanning 530001, China;School of Chemistry and Chemical Engineering, SUN YAT-SEN University, Guangzhou 510275, China;College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China;Clinical Chemistry Program, Department of Chemistry, SI 424, Cleveland State University, Cleveland, OH 44115, USA

关键词: pregnenolone;    17-acetamidoandrostane;    N;    N-dimethyl-7-deoxycholic amide;    antiproliferative activity;   

DOI  :  10.3390/molecules18077436

来源: mdpi

【 摘 要 】

Using pregnenolone and 7-deoxycholic acid as starting materials, some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives were synthesized. The cytotoxicity of the synthesized compounds was tested in vitro against two tumor cell lines: SGC 7901 (human gastric carcinoma) and Bel 7404 (human liver carcinoma). The result showed that the blockage of the interaction of the amide group with outside groups might cause a decrease of the cytotoxicity, and an O-benzyloximino group at the 3-position of N,N-dimethyl-7-deoxycholic amide could enhance the cytotoxic activity of the compound. The information obtained from the studies provides the structure-activity relationship for these compounds and may be useful for the design of novel chemotherapeutic drugs.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.