双氯芬酸酰胺衍生物作为潜在抗肿瘤药物的合成及生物学评价
Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-tumor agents.
作者信息
Zhong Guang-Xiang, Chen Lu-Lu, Li Hai-Bo, Liu Fu-Jin, Hu Jin-Qing, Hu Wei-Xiao
机构信息
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032, PR China.
出版信息
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4399-402. doi: 10.1016/j.bmcl.2009.05.082. Epub 2009 May 24.
To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition growth rate of human lung cancer cell (A549) and human endometrial adenocarcinoma cell (Ishikawa) in vitro was evaluated. The preliminary assay results showed that compounds 6j, 7o and 8c exhibited good anti-tumor activities and excellent selectivity for the Ishikawa cell, may be potential anti-tumor agents.
为发现新的药用活性，对二氟尼柳的结构进行了修饰。以二氟尼柳为起始原料，分三步合成了40种二氟尼柳的酰胺衍生物。评估了它们在体外对人肺癌细胞（A549）和人子宫内膜腺癌细胞（Ishikawa）的抑制生长率。初步测定结果表明，化合物6j、7o和8c表现出良好的抗肿瘤活性，对Ishikawa细胞具有优异的选择性，可能是潜在的抗肿瘤药物。
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