82257-37-2Relevant 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.
Microwave-assisted synthesis of some substituted sulfamides
Gediz Erturk, Aliye,Bekdemir, Yunus
, p. 285 - 292 (2014/01/06)
Microwave-assisted synthesis of some substituted open-chain and cyclic sulfamides, by amine-exchange reaction, was studied in a modified domestic microwave oven. Reaction times and yields under microwave radiation were compared with classical heating. Synthesis of the sulfamides under microwave irradiation gave better yields with the desired compounds, and in considerably reduced reaction times, than those obtained by classical heating. [Supplementary materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfer, and Silicon and the Related Elements for the following free supplemental files: Additional figures.]