标题：Novel aminopeptidase N (APN/CD13) inhibitors derived from chloramphenicol amine.
作者：Jia M;Yang K;Fang H;Xu Y;Sun S;Su L;Xu W
作者机构：[Jia, M] Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, Ji'nan, Shandong 250012, China;[ Yang, K] D 更多
通讯作者地址：[Xu, WF]Shandong Univ, Sch Pharm, Dept Med Chem, 44 W Culture Rd, Jinan 250012, Shandong, Peoples R China.
来源：Bioorganic and medicinal chemistry
关键词：Aminopeptidase N inhibitors; Chloramphenicol amine derivatives;; Synthesis; QSAR
摘要：Aminopeptidase N (APN) is involved in different physiological and pathological processes of tumor cells, including proliferation, invasion, apoptosis and metastasis. Herein one series of compounds derived from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol have been designed and synthesized. Furthermore, preliminary activity evaluation showed that some compounds elicited moderate inhibitory activity against APN with compounds 10e (IC(50)=6.1+/-0.5 muM) possessing the best efficacy, which could be used as the lead compound in the future for anticancer agents research.