Design, synthesis and biological evaluation of novel nitroaromatic compounds as potent glutathione reductase inhibitors
[ X ]
Tarih
2011
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Pergamon-Elsevier Science Ltd
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Discovery of GR inhibitors has become very popular recently due to antimalarial and anticancer activities. In this study, the synthesis and GR inhibitory capacities of novel nitroaromatic compounds (NCs) (1-3) were reported. Some commercially available molecules were also tested for comparison reasons. The novel NCs were obtained in high yields using simple chemical procedures and exhibited much potent inhibitory activities against GR at low micromolar concentrations with K-i values ranging from 0.211 to 4.57 mu M as compared with well-known agents. Inhibition mechanism was assessed as being due to occlusion of the active site entrance by means of the NCs. Molecular docking results have shown that docking poses of ligands are able to construct binding interactions with the essential amino acids. (C) 2011 Elsevier Ltd. All rights reserved.
Açıklama
Anahtar Kelimeler
Glutathione Reductase, Antimalaria, Nitroaromatic, In Silico Docking
Kaynak
Bioorganic & Medicinal Chemistry Letters
WoS Q Değeri
Q2
Scopus Q Değeri
Q2
Cilt
21
Sayı
18
