Literature DB >> 18571419

Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold.

GuoGang Tu1, ShaoHua Li, HuiMing Huang, Gang Li, Fang Xiong, Xi Mai, HuaWei Zhu, BinHai Kuang, Wen Fang Xu.   

Abstract

The aminopeptidase N (APN/CD13), overexpressed in tumor cells, plays a critical role in angiogenesis. In this study, we report the synthesis and in vitro enzyme inhibition assay of 1,3,4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC(50) values in the micromol rang.

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Year:  2008        PMID： 18571419     DOI： 10.1016/j.bmc.2008.05.081

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  7 in total

1.  (2R,3R)-N-(4-Chloro-phen-yl)-2,3-dihydr-oxy-N'-(5-phenyl-1,3,4-thia-diazol-2-yl)succinamide.

Authors:  Hui-Ming Huang; Gen-Lin Chen; Min Li; Guo-Gang Tu; Cheng-Mei Liu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-03-06

2.  (2R)-N-[5-(4-Chloro-phen-yl)-1,3,4-thia-diazol-2-yl]-2-(cinnamoylamino)propanamide.

Authors:  Shao-Hua Li; Hui-Ming Huang; Bin-Hai Kuang; Guo-Gang Tu; Cheng-Mei Liu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-09-24

3.  4-Chloro-N-[3-methyl-1-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)but-yl]benzamide.

Authors:  Yu-Gang Yan; Guo-Gang Tu; Ling-Dong Wang; Jian Liu; Shao-Hua Li
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-05-19

4.  (2R)-2-Cinnamoylamino-N-[5-(4-methoxy-phen-yl)-1,3,4-thia-diazol-2-yl]propanamide.

Authors:  Shao-Hua Li; Gang Li; Hui-Ming Huang; Guo-Gang Tu; Cheng-Mei Liu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-09-06

5.  2-Benzoyl-amino-N-[5-(4-bromo-phen-yl)-1,3,4-thia-diazol-2-yl]ethanamide.

Authors:  Hui-Ming Huang; Shi-Yuan Luo; Shao-Hua Li; Cheng-Mei Liu; Guo-Gang Tu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-01-17

6.  Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors.

Authors:  Kanghui Yang; Qiang Wang; Li Su; Hao Fang; Xuejian Wang; Jianzhi Gong; Binghe Wang; Wenfang Xu
Journal:  Bioorg Med Chem       Date:  2009-04-24       Impact factor: 3.641

7.  2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase.

Authors:  Ilkay Küçükgüzel; Gökhan Satılmış; K R Gurukumar; Amartya Basu; Esra Tatar; Daniel B Nichols; Tanaji T Talele; Neerja Kaushik-Basu
Journal:  Eur J Med Chem       Date:  2013-09-12       Impact factor: 6.514
  7 in total

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