期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 66, 期 -, 页码 438-449出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.06.015
关键词
Alkaline phosphatase inhibitors; Ecto-5 '-nucleotidase inhibitors; Chromones; Sulfonamides; Molecular docking; Structure activity relationships (SARs)
资金
- PhD scholarship (HEC Indigenous 5000 PhD Fellowship Program, Batch-III)
- COMSTECH-TWAS
- German-Pakistani Research Collaboration Programme
- Canadian Institutes of Health Research
A new series of structurally diverse chromone containing sulfonamides has been developed. Crystal structures of three representative compounds (2a, 3a and 4a) in the series are reported. All compounds were screened for their inhibitory potential against alkaline phosphatases (ALPs). Two main classes of ALP isozymes were selected for this study, the tissue non-specific alkaline phosphatase (TNALP) from bovine and porcine source and the tissue-specific intestinal alkaline phosphatases (IALPs) from bovine source. All sulfonamide compounds had a marked preference for IALP (K-i, up to 0.01 +/- 0.001 mu M) over TNALPs. Kinetics studies of the compounds showed competitive mode of inhibition. Molecular docking studies were carried out in order to characterize the selective inhibition of the compounds. An additional interesting aspect of these chromone sulfonamides is their inhibitory activity against ecto-5'-nucleotidase enzyme. (C) 2013 Elsevier Masson SAS. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据