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

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

  • Biosci Rep. 2018 Feb 13;38(1):BSR20171440. doi: 10.1042/BSR20171440.
Huan-Huan Sha 1,  Zhen Wang 2,  Shu-Chen Dong 1,  Tian-Mu Hu 3,  Si-Wen Liu 4,  Jun-Ying Zhang 4,  Yang Wu 4,  Rong Ma 4,  Jian-Zhong Wu 4,  Dan Chen 4,  Ji-Feng Feng 5
Affiliations

Affiliations

  • 1 The Fourth Clinical School of Nanjing Medical University and Nanjing Medical University Affiliated Cancer Hospital, Baiziting42, Nanjing 210009, China.
  • 2 The First Clinical School of Nanjing Medical Universityand Department of Orthopedics, the First Affiliated Hospital of Nanjing Medical University, Guangzhou Road300, Nanjing 210009, China.
  • 3 Department of Biological Science, Purdue University, West Lafayette, IN 47906, U.S.A.
  • 4 Jiangsu Cancer Hospital and Jiangsu Institute of Cancer Research and Nanjing Medical University Affiliated Cancer Hospital, Baiziting42, Nanjing 210009, China.
  • 5 Jiangsu Cancer Hospital and Jiangsu Institute of Cancer Research and Nanjing Medical University Affiliated Cancer Hospital, Baiziting42, Nanjing 210009, China jifeng_feng@163.com.
PMID: 29358310 DOI: 10.1042/BSR20171440
Abstract

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.

Keywords

GSTP1-1 (Glutathione S-transferase Pi); JNK (c-Jun N-Terminal Kinase); NBDHEX (6- (7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol); anticancer.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z