Author/Authors :
Andrea Guiotto، نويسنده , , Mirta Canevari، نويسنده , , Piero Orsolini، نويسنده , , Olivier Lavanchy، نويسنده , , Christine Deuschel، نويسنده , , Norimasa Kaneda، نويسنده , , Akinobu Kurita، نويسنده , , Takeshi Matsuzaki، نويسنده , , Takeshi Yaegashi، نويسنده , , Seigo Sawada، نويسنده , , Francesco M. Veronese، نويسنده ,
Abstract :
A new poly(ethylene glycol) (PEG) conjugate of 10-amino-7-ethyl camptothecin, a potent antitumor analogue of camptothecin, has been synthesized and preliminary in vivo tests have been performed. Successful chemoselective N-acylation of 10-amino-7-ethyl camptothecin was accomplished using phenyl dichlorophosphate, a coupling reagent used in esterification of alcohols, while other coupling methods failed, due to the low nucleophilicity of the amino group in position 10. The conjugate was tested against P388 murine leukemia cell lines and resulted equipotent to CPT-11, a camptothecin analogue already in clinical use.
Keywords :
PEG , camptothecin , Phenyl dichlorophosphate. , conjugation
