Study On Synthesis Of S-Tetrazine Derivatives And Their Structure-Activity Relationships Of Anti-tumour

We obtained a series of Chloro-substituent hydrazone and S-tetrazine derivatives via the method of Chloro-substituent hydrazone.All the compounds were confirmed by HNMR, IR, MS and EA. The space configuration of two S-tetrazine derivatives were confirmed by X-Ray diffraction.The paper included three parts: (1) synthesis a seris of phenyl hydrazone derivatives via the reaction of aldehyde and substituent hydrazine ;then obtained α-chloro-phenylhydrazone derivatives via chlorine. Seven new compounds 1,4-dihydrotetrazine-1,4-dicarbonate were obtained via reaction of N-substituent-α-Chloro-phenylhydrazone Derivatives and triethylamine in THF solvent. (2) first, synthesis N-substitent semicarbazide derivatives, phenyl hydrazone derivatives were obtained by the reaction of aldehyde and N-substitent semicarbazide;then we got six newa-Chloro-phenylhydrazone derivatives and two new S-tetrazine derivatives by the same method of Part (1). (3) X-ray diffraction determined the Single crystals of two compounds synthesized before ,and the space configurarion are confirmed .The antitumor activity of these compounds against P-388 and A-549 in vitro were tested by The Nation Center for Drug Screening in Shang Hai. The results showed that antitumor activity was considered as a weak...