Synthesis and Characterization of Hypoxia Actived Prodrug of Triptolide
(OBJECTIVE)The hypoxia actived prodrug of triptolide was synthesized,and its structure was confirmed.Additionally,two con-trol compounds Gem1 and Dox1 were prepared.In total,three Hypoxia actived prodrugs were obtained in order to further antitumor study.(METHOD)We used 2-nitroimidazole as the starting material.Subsequently,3-(2-nitro-1H-imidazole-1-yl)propionic acid has been yielded through nucleophilic substitution and hydrolysis.The target compounds,Gem1 and Dox1 were obtained by condensation reaction of 3-(2-nitro-1H-imidazol-1-yl)propionic acid with triptolide,doxorubicin,and gemcitabine,respectively.And their structures were confirmed using 1H-NMR and high-resolution mass spectrometry.(RESULTS)we successfully obtained the target compound and Dox1 and Gem1.(CONCLUSION)the structures of target compound and Dox1 and Gem1 were confirmed by 1H-NMR and high-resolution mass spectrometry.Three hypoxia activated prodrugs were successfully obtained in order to do further antitumor studies.
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