Synthesis and antitumor activity of 20-O-linked camptothecin ester derivatives

AimTo improve the profile of 20(S)-camptothecin, a series of 20-O-linked camptothecin phenoxyacetic acid ester derivatives have been designed. MethodsThese derivatives were synthesized by the method of acylation. Their chemical structures were confirmed with ¹HNMR, IR, MS, and HRMS. The cytotoxicities of the compounds were tested by MTT assay. The in vivo antitumor activities of these esters were evaluated against mouse liver tumor H₂₂ in mice. ResultsTwelve derivatives of camptothecin ester are new compounds. Conclusionin vitro and in vivo antitumor activity has indicated that some derivatives appeared significantly more effective than topotecan in the H₂₂ mouse liver tumoral model.