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Design, Synthesis, and Activity Evaluation of a New 5-fluorouracil Prodrug Containing an Asn-Gly-Arg(NO2)COOCH3 Tripeptide

[ Vol. 19 , Issue. 10 ]


Yepeng Luan, Fanbo Jing, Jian Zhang, Mingming Zou, Xuejian Wang, Yuping Jia, Ning Liu, Jiajia Mou and Wenfang Xu   Pages 1122 - 1131 ( 10 )


Aminopeptidase N (APN/CD13) of the M1 family is a broad specificity enzyme that is intimately involved in tumor angiogenesis and metastasis. Asparagine–glycine–arginine (NGR) is a tumor-homing tripeptide, which can selectively combine with APN/CD13 that is overexpressed on the surface of some tumor cells. Various anti-tumor drugs can be conjugated to NGR to improve selectivity, efficacy, and to decrease drug toxicity. In this study, a tripeptide NGR(NO2) was synthesized and conjugated with 5-fluorouracil. The anti-tumor activities of this new prodrug were evaluated in vivo. More significant anti-tumor effects were observed over the parent 5-fluorouracil.


Aminopeptidase N, NGR, 5-fluorouracil, antitumor, angiogenesis, metastasis, tumor cells, tumor-homing tripeptide, 5-fluorouracil


Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan, Shandong, 250012, China.

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