Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis

Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis

The antitumor agent 6-((7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio)hexan-1-ol (1) is a potent inhibitor of GSTP1-1, a glutathione S-transferase capable of inhibiting apoptosis by binding to JNK1 and TRAF2. We recently demonstrated that, unlike its parent compound, the benzoyl ester of 1 (compound 3)...

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Bibliographic Details
Main Authors: Veronica Di Paolo, Chiara Fulci, Dante Rotili, Francesca Sciarretta, Alessia Lucidi, Blasco Morozzo della Rocca, Anastasia De Luca, Antonio Rosato, Luigi Quintieri, Anna Maria Caccuri
Format: Article
Language:English
Published: Taylor & Francis Group 2019-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
nitrobenzoxadiazoles
gstp1-1
traf2
glutathione
a375 human melanoma
Online Access:http://dx.doi.org/10.1080/14756366.2019.1617287

Internet

http://dx.doi.org/10.1080/14756366.2019.1617287

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