436091-88-2Relevant articles and documents
Amino-(N-alkyl) benzsulfamide synthesis method
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Paragraph 0121-0124, (2017/04/14)
The invention discloses an amino-(N-alkyl) benzsulfamide synthesis method. The method comprises the steps of adding aminobenzenesul fonamide, an iridium complex catalyst, alkali, compound alcohol and the solvent tert-amyl alcohol into a reaction container for reaction lasting several hours at 120-150 DEG C, then reducing temperature to room temperature, conducting rotary evaporation to remove the solvent, and then conducting column separation to obtain the target compound. Commercial aminobenzenesul fonamide and nearly non-toxic compound alcohol are used as starting materials, only water is generated as reaction byproduct, and no environment harm is done; reaction atom economy is high.
Synthesis and biological evaluation of norcantharidin derivatives as protein phosphatase-1 inhibitors
Zhao, Jie,Guan, Xiao-Wen,Chen, Shi-Wu,Hui, Ling
, p. 363 - 366 (2015/02/19)
Cantharidin and norcantharidin display anticancer activity against a broad range of tumor cell lines. In this study, we have synthesized a series of norcantharidin derivatives and evaluated their cytotoxic effects on four human tumor cell lines together with the genetically normal human diploid fibroblast line WI-38. One of our compounds (1S,4R)-3-((4-(4-(4-fluorophenyl)piperazin-1-ylsulfonyl) phenyl)carbamoyl)-7-oxa-bicyclo[2.2.1]heptane-2-carboxylic acid (12) exhibited potent cytotoxic effects on the tumor cell lines A-549, HepG2, HeLa, and HCT-8, whereas it was less toxic to WI-38 cells than its parent compound, norcantharidin. In addition, this compound inhibited protein phosphatase-1 activity and microtubule formation in HeLa cells, and it also interacts with calf thymus DNA.