35455-36-8Relevant academic research and scientific papers
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I)
Li, Xun,Wang, Junli,Li, Jinpei,Wu, Jifeng,Li, Yonggang,Zhu, Huawei,Fan, Ruifang,Xu, Wenfang
, p. 3053 - 3060 (2009)
Overexpression of zinc-dependent metalloproteinase, aminopeptidase N (APN/CD13), is considered to be involved in the process of tumor invasion and metastasis. Herein we describe the synthesis and in vitro enzymatic inhibition assay of antineoplaston AS2-5 scaffold peptidomimetic compounds. The results demonstrated that most of these l-iso-glutamine derivatives displayed selective inhibitory activity against APN as compared with MMP-2, with IC50 values in the micromole range. The structure-activity relationships were also briefly discussed.
Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Design, chemistry and activity evaluation. Part I
Li, Qianbin,Fang, Hao,Wang, Xuejian,Hu, Liping,Xu, Wenfang
experimental part, p. 4819 - 4825 (2010/02/27)
A series of aminopeptidase inhibitors with cyclic-imide scaffold are described. The biological characterization for the piperidinedione analogues revealed that most compounds displayed high inhibitory activity against APN. Among which 4l and 6 showed pote
Structure confirmation of L-iso-glutamine derivatives
Li, Xun,Xu, Wen-Fang
, p. 94 - 95 (2007/10/03)
L-iso-glutamine derivatives as an APNIs was prepared by the condensation reaction of N-(3,4,5-trimethoxybenzoyl)-glutamic acid anhydride with L-amino acid methyl ester hydrochloride. The structure was confirmed by MS, Elemental and X-ray single crystal diffraction.
New glutamic and aspartic derivatives with potent CCK-antagonistic activity
Makovec,Chiste,Bani,et al.
, p. 9 - 20 (2007/10/02)
New derivatives of aspartic and glutamic acid were synthesized and evaluated in vitro and in vivo for anti-CCK activity on the guinea pig gallbladder. The anti-CCK activity of some 4-benzamido-glutaramic acid derivatives was a hundred times greater than that of proglutamide, the model compound, and they have been selected for further studies.
