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

• Main Authors: Veronica Di Paolo (Author), Chiara Fulci (Author), Dante Rotili (Author), Francesca Sciarretta (Author), Alessia Lucidi (Author), Blasco Morozzo della Rocca (Author), Anastasia De Luca (Author), Antonio Rosato (Author), Luigi Quintieri (Author), Anna Maria Caccuri (Author)
• Format: Book
• Published: Taylor & Francis Group, 2019-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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)...