Studies on water-soluble taxol derivatives

The importance of taxol as an anticancer drug lies not only in its activity in antitumor assays but also in its unique mechanism of action. Unfortunately, taxol is not water-soluble and therefore must be given in conjunction with emulsifying agents. Modifications of taxol were carried out in order to prepare water-soluble taxol derivatives. The C-2’ hydroxyl group of taxol was substituted with various groups to increase water solubility. The synthesized taxol derivatives, 2’-((3-sulfo-1-oxopropyl)oxy)taxol sodium salt, 2’-((4-((2-sulfoethyl)amino)-1,4-dioxobutyl)oxy)taxol sodium salt, and 2’-((4-((3-sulfopropyl)amino)-1,4-dioxobutyl)oxy)taxol sodium salt were more water-soluble than taxol. The synthetic pathways to these compounds are compared and discussed.