Synthesis and cytotoxic activity on islets of Langerhans of benzamide thiosemicarbazone derivatives
                                
                                    
                                        作者:M Campana、C Laborie、G Barbier、R Assan、R Milcent                                    
                                    
                                        DOI:10.1016/0223-5234(91)90059-v
                                    
                                    
                                        日期:1991.4
                                    
                                    Eleven 1-(4-substituted alpha-arylaminobenzylidene)thiosemicarbazides 1 and the related semicarbazones 2 were synthesized and tested in vitro for their inhibitory effects on the islets of Langerhans.  Only the thiosemicarbazones 1 suppressed the insulin and glucagon secretions while the somatostatin release persisted.  The 1-(alpha-anilino-4-methylbenzylidene)thiosemicarbazide 1f was the most potent suppressor of insulin release and lysed the islet beta cells.  Zinc sulfate protected islets from the suppressive and toxic effects of 1f.  These compounds 1 could be potential drugs for the treatment of insulinomas.