Tasisulam is a promising antitumor agent with complex pharmacology, which is used as an antiproliferative agent in patients with metastatic melanoma and other solid tumors. Phase 2 melanoma studies showed promising results but had to be stopped because of insufficient tasisulam clearance leading to toxic side effects. To reduce the negative effects of tasisulam, we synthesized a novel sulfonimidamide-based analog to evaluate its antiproliferative effects in comparison to the original compound by performing a cell proliferation assay in melanoma cell lines SKMel23 and A375. The results revealed that the analog had inhibitory effects on the proliferation comparable to tasisulam in both investigated cell lines. These results could contribute to a reduced toxicity of tasisulam and lead to further clinical trials in metastatic melanoma.
Electrochemical technologies for the treatment of industrial and municipal wastewaters, potable water, and groundwater, are presented, focusing on the main water constituents: inorganics, organics, micropollutants, and microorganisms. Removal of inorganic compounds by electrodialysis, electrocoagulation, and capacitive deionization as well as removal of organics and micropollutants by electrosorption, advanced oxidation processes, and anodic oxidation with boron‐doped diamond electrodes are reviewed. Electricity can be generated by degradation of organic compounds in microbial fuel cells and dehalogenation by cathodic reduction minimizes toxic substances in water. The disinfection of different types of water is also presented and it is shown that electrochemical methods offer versatile approaches to contribute to an sustainable future water management.
The application of borylated N-aryl sulfoximines as newly designed synthetic building blocks in Suzuki-type cross coupling reactions offers rapid access to a wide range of N-biaryl derivatives with potential relevance for medicinal chemistry and crop protection in good to excellent yields (up to 98%).
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