Synthesis Research Of Two Kinds Of Water-Soluble Camptothecin Derivatives

Camptothecin and some of its derivatives, in the target of inhibitors of topoisomerase I, have strong antitumor activity. The 10-hydroxycamptothecin(HCPT) demonstrates more significant antitumor activity and less toxicity than another natural alkaloid—the camptothecin, so it arrests more and more attention as an important intermediate in camptothecin derivatives. For the poor water-solubility, however, HCPT is generally applied in the clinic in the form of a soluble sodium salt that will lead invalidation over 90% medicament because of the hydrolyzation of E-ring lactones. And the increased dosage will raise the risk of toxicity. So it is so important to modify HCPT locally to improve its water-solubility in order to overcome invalidation problem.It was first put forward in this paper that the phosphorylation and the glucosidation modification in 10-hydroxyls of HCPT in which water-solubility phosphoryl and glucopyranoside groups were introduced in and two novel water-solubility camptothecin derivatives were synthesizedIn this paper, a new HCPT phosphate diester derivative with the same...