1615-08-3Relevant articles and documents
Towards the inhibition of protein–protein interactions (PPIs) in STAT3: Insights into a new class of benzothiadiazole derivatives
Asai, Akira,Colombo, Diego,Gelain, Arianna,Gilardoni, Ettore,Meneghetti, Fiorella,Mori, Matteo,Parkinson, Gary,Pedretti, Alessandro,Regazzoni, Luca,Villa, Stefania
, (2020/08/28)
Signal transducer and activator of transcription 3 (STAT3) is a validated anticancer target due to the relationship between its constitutive activation and malignant tumors. Through a virtual screening approach on the STAT3-SH2 domain, 5,6-dimethyl-1H,3H-2,1,3-benzothiadiazole-2,2-dioxide (1) was identified as a potential STAT3 inhibitor. Some benzothiadiazole derivatives were synthesized by employing a versatile methodology, and they were tested by an AlphaScreen-based assay. Among them, benzosulfamide 1 showed a significant activity with an IC50 = 15.8 ± 0.6 μM as a direct STAT3 inhibitor. Notably, we discovered that compound 1 was also able to interact with cysteine residues located around the SH2 domain. By applying mass spectrometry, liquid chromatography, NMR, and UV spectroscopy, an in-depth investigation was carried out, shedding light on its intriguing and unexpected mechanism of interaction.
Vicinal Diamination of Arenes with Domino Aryne Precursors
Li, Lu,Qiu, Dachuan,Shi, Jiarong,Li, Yang
, p. 3726 - 3729 (2016/08/16)
Vicinal diamination of domino aryne precursors was achieved with sulfamides. The reaction proceeds through a two-aryne pathway, accepting two N-nucleophiles at the 1,2-positions of an arene ring. Symmetrical and unsymmetrical diaminobenzenes were readily obtained.
