Design, Synthesis and Preliminary Activity Evaluation of Novel L-Lysine Derivatives as Aminopeptidase N/CD13 Inhibitors

Qiang      Wang; Fuming      Xu; Jiajia      Mou; Jian      Zhang; Luqing      Shang; Yepeng      Luan; Yumei      Yuan; Yingzi      Liu; Minyong      Li; Hao      Fang; Binghe      Wang; Wenfang      Xu

doi:10.2174/092986610791306661

Abstract

A novel class of L-lysine derivatives as aminopeptidase N (APN) inhibitors was designed and synthesized. Activity evaluation showed that compound C7 (IC50 = 9.6 ± 1.3 μM) and C20 (IC50 = 13.6 ± 1.9 μM) were equivalent to the positive control Bestatin (IC50 = 11.3 ± 1.6 μM).

Keywords: Lysine derivatives, Synthesis, APN, Inhibitor

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Protein & Peptide Letters

Title: Design, Synthesis and Preliminary Activity Evaluation of Novel L-Lysine Derivatives as Aminopeptidase N/CD13 Inhibitors

Volume: 17 Issue: 7

Author(s): Qiang Wang, Fuming Xu, Jiajia Mou, Jian Zhang, Luqing Shang, Yepeng Luan, Yumei Yuan, Yingzi Liu, Minyong Li, Hao Fang, Binghe Wang and Wenfang Xu

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Keywords: Lysine derivatives, Synthesis, APN, Inhibitor

Abstract: A novel class of L-lysine derivatives as aminopeptidase N (APN) inhibitors was designed and synthesized. Activity evaluation showed that compound C7 (IC50 = 9.6 ± 1.3 μM) and C20 (IC50 = 13.6 ± 1.9 μM) were equivalent to the positive control Bestatin (IC50 = 11.3 ± 1.6 μM).

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Wang Qiang, Xu Fuming, Mou Jiajia, Zhang Jian, Shang Luqing, Luan Yepeng, Yuan Yumei, Liu Yingzi, Li Minyong, Fang Hao, Wang Binghe and Xu Wenfang, Design, Synthesis and Preliminary Activity Evaluation of Novel L-Lysine Derivatives as Aminopeptidase N/CD13 Inhibitors, Protein & Peptide Letters 2010; 17 (7) . https://dx.doi.org/10.2174/092986610791306661