| 초록 |
Camptothecin (CPT) is a plant alkaloid isolated from Camptotheca acuminata with a significant antitumor activity against a variety of human solid tumors. Its clinical application is limited by insolubility in water and instability at neutral pH. In in vivo and aqueous buffer solutions, CPT rapidly converts into pharmacologically less active carboxylate form. A common prodrug strategy to stabilize the active lactone form of CPT is by Esterification at 20-OH of CPT. In this study, a mean to deliver soluble and active CPT was carried out. A prodrug of CPT was synthesized by coupling a glycine moiety into the 20-OH of CPT. This prodrug was reacted with cyclotriphosphazene which was firstly substituted with methoxy-poly(ethylene glycol) (MPEG). The structure of this prodrug conjugate, along with its physical property and in vitro cytotoxicity were evaluated. |
