714972-07-3

Basic information

• Product Name: 4-(2-isothiocyanatoethyl)benzenesulfonamide
• Synonyms: 4-(2-isothiocyanatoethyl)benzenesulfonamide
• CAS NO: 714972-07-3
• Molecular Weight: 242.323
• Mol File: 714972-07-3.mol

Chemical Properties

• CAS DataBase Reference: 4-(2-isothiocyanatoethyl)benzenesulfonamide(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(2-isothiocyanatoethyl)benzenesulfonamide(714972-07-3)
• EPA Substance Registry System: 4-(2-isothiocyanatoethyl)benzenesulfonamide(714972-07-3)

Safety Data

• Hazardous Substances Data: 714972-07-3(Hazardous Substances Data)

Upstream product

• 75-15-0 carbon disulfide 
• 35303-76-5 4-(2-aminoethyl)benzenesulfonamide 

Downstream Products

• 1383371-00-3 N-(4-sulfamoylphenylethyl)-N-((2-aminoethyl)-2-methyl-5-nitroimidazolyl)thiourea 

Relevant articles and documents

Fluorescent Silica Nanoparticles with Multivalent Inhibitory Effects towards Carbonic Anhydrases

Multifunctional silica nanoparticles decorated with fluorescent and sulfonamide carbonic anhydrase (CA) inhibitors were prepared and investigated as multivalent enzyme inhibitors against the cytosolic isoforms hCA I and II and the transmembrane tumor-asso

Synthesis 4-[2-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-ethyl]-benzenesulfonamides with subnanomolar carbonic anhydrase II and XII inhibitory properties

Condensation of substituted anthranilic acids with 4-isothiocyanatoethyl-benzenesulfonamide led to series of heterocyclic benzenesulfonamides incorporating 2-mercapto-quinazolin-4-one tails. These sulfonamides were investigated as inhibitors of the human

Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors

Multi-target, especially dual-target, drug design has become a popular research field for cancer treatment. Development of small molecule dual-target inhibitors through hybridization strategy can provide highly potent and selective anticancer agents. In this study, three series of quinazoline derivatives bearing a benzene-sulfonamide moiety were designed and synthesized as dual EGFR/CAIX inhibitors. All the synthesized compounds were evaluated against epidermoid carcinoma (A431) and non-small cell lung cancer (A549 and H1975) cell lines, which displayed weak to potent anticancer activity. In particular, compound 8v emerged as the most potent derivative against mutant-type H1975 cells, which exhibited comparable activity to osimertinib. Importantly, 8v exhibited stronger anti-proliferative activity than osimertinib against H1975 cells under hypoxic condition. Kinase inhibition studies indicated that 8v showed excellent inhibitory effect on EGFRT790M enzyme, which was 41 times more effective than gefitinib and almost equal to osimertinib. Mechanism studies revealed that 8v exhibited remarkable CAIX inhibitory effect comparable to acetazolamide and significantly inhibited the expression of p-EGFR as well as its downstream p-AKT and p-ERK in H1975 cells. Notably, 8v was found to inhibit the expression of CAIX and its upstream HIF-1α in H1975 cells under hypoxic condition. Molecular docking was also performed to gain insights into the ligand-binding interactions of 8v inside EGFRWT, EGFRT790M and CAIX binding sites.

Novel derivatives of benzimidazole and imidazo-pyridine and their use as medicaments

A compound of the formula wherein the substituents are as defined in the specification and pharmaceutical salts thereof having a good affinity for sub-types of melanocortin receptors making them useful for treating diseases in which such receptors are included such as pain, inflammatory conditions, etc.