abstract |
Disclosed are water-soluble camptothecin prodrugs as represented by formula (2) or (3), or a pharmaceutically acceptable salt, or a hydrate or solvate thereof, wherein in Formula (2), R1 represents a hydrogen atom or an alkyl group; X represents a C=O or an alkylene group; R2 and R4 each independently represents a hydrogen atom, an alkyl group, or an amino acid side chain; and R3 represents an alkyl group; wherein in Formula (3), R1 is defined as in formula (2); n represents an integer from 1 to 6; and R5 represents a hydrogen atom or COOR6 (wherein R6 represents a hydrogen atom or an alkyl group); wherein in Formula (2) and (3), Y is a group represented by formula (5): and the other substituents are as defined herein. Also disclosed is a therapeutic agent for a cell proliferation disorder (such as colorectal cancer, lung cancer, breast cancer, gastric cancer, uterine cervical cancer, bladder cancer or a solid tumor) which comprises the water-soluble prodrug as defined above as an effective ingredient. |