6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound

The 7-nitro-2,1,3-nitrobenzoxadiazole (NBD) derivatives are a series of compounds containing the NBD scaffold that are not glutathione (GSH) peptidomimetics, and result in a strong inhibition of glutathione S-transferases (GSTs). Growing evidences highlight their pivotal roles and outstanding antica...

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Veröffentlicht in:Bioscience reports 2018-02, Vol.38 (1)
Hauptverfasser: Sha, Huan-Huan, Wang, Zhen, Dong, Shu-Chen, Hu, Tian-Mu, Liu, Si-Wen, Zhang, Jun-Ying, Wu, Yang, Ma, Rong, Wu, Jian-Zhong, Chen, Dan, Feng, Ji-Feng
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container_title Bioscience reports
container_volume 38
creator Sha, Huan-Huan
Wang, Zhen
Dong, Shu-Chen
Hu, Tian-Mu
Liu, Si-Wen
Zhang, Jun-Ying
Wu, Yang
Ma, Rong
Wu, Jian-Zhong
Chen, Dan
Feng, Ji-Feng
description The 7-nitro-2,1,3-nitrobenzoxadiazole (NBD) derivatives are a series of compounds containing the NBD scaffold that are not glutathione (GSH) peptidomimetics, and result in a strong inhibition of glutathione S-transferases (GSTs). Growing evidences highlight their pivotal roles and outstanding anticancer activity in different tumor models. In particular, 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol (NBDHEX) is extensively studied, which is a very efficient inhibitor of GSTP1-1. It triggers apoptosis in several tumor cell lines and this cytotoxic activity is observed at micro and submicromolar concentrations. Importantly, studies have shown that NBDHEX acts as an anticancer drug by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. Additionally, some researchers also have discovered that NBDHEX can act as late-phase autophagy inhibitor, which opens new opportunities to fully exploit its therapeutic potential. In this review, we summarize the advantages, anticancer mechanisms, and analogs of this compound, which will establish the basis on the usage of NBDHEX in clinical applications in future.
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In this review, we summarize the advantages, anticancer mechanisms, and analogs of this compound, which will establish the basis on the usage of NBDHEX in clinical applications in future.</abstract><cop>England</cop><pub>Portland Press Ltd The Biochemical Society</pub><pmid>29358310</pmid><doi>10.1042/bsr20171440</doi><oa>free_for_read</oa></addata></record>
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subjects Anticancer properties
Antineoplastic drugs
Antitumor activity
Apoptosis
Autophagy
Bone cancer
Catalytic activity
Cell cycle
Cytotoxicity
Drug interactions
Drug resistance
Glutathione
Glutathione transferase
Hexanol
Inhibitors
Kinases
Leukemia
Melanoma
Mesothelioma
Peptidomimetics
Phosphorylation
Proteins
Review
Sarcoma
Signal transduction
Tumor cell lines
Tumors
title 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound
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