10-hydroxycamptothecin (10-HCPT) is a camptothecin analogue with a powerful cytotoxic effect for cancer therapies. Increasing attention has been paid on the synthesis and pharmacological activities of 10-HCPT and its derivatives. In the study, the design, synthesis and biological evaluation of 10-HCPT derivative was researched. The newly synthesized 10-HCPT derivative was characterized by 1H-NMR and the anticancer activity was also investigated by MTT assay and in vivo test. MTT results suggested that the new compound has better biological effect than 10-HCPT on four tumor cell lines including K562, HT-29, HepG2 and S180. The new compound also showed good inhibition on S180 ascites model.