To produce the subject new water-soluble ands relatively nontoxic prodrug, comprising paclitaxel bonded to a cleavable N-(aliphatic or an aromatic)-O-glycosyl carbamate spacer group and useful for treatment, etc., of cancer.
This new paclitaxel prodrug (salt) comprises paclitaxel bonded to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group and is represented by formula I [R1 to R3 are each H or CH3; R4 is a group represented by CH2OH or C(O)O-Z+ (Z is H, Li, Na or K)] or formula II [R5 is H or a group represented by CX3 (X is a halogen) or OY (Y is a 1-3C alkyl or an aryl); (n) is 1 or 2] and is useful for treatment, etc., of cancer. The compound can be obtained by reacting a carboxylic acid compound including a carbohydrate having a protected hydroxyl group with a compound represented by formula III, forming an ester and then carrying out the deprotection of the carbohydrate.
LEENDERS RUBEN G G (NL)
SCHEEREN JOHAN W (NL)
HAISMA HIDDE J (NL)
DE VOS DICK (NL)
