Search

Based on a new semisynthetic route, a series of phosphotriester 7-alkyl-homocamptothecin derivatives are designed and synthesized. Cytotoxic activity assays show that compounds 12a and 14c with a methyl in position C7 of the homocamptothecin are more potent than the other derivatives and the positive drug irinotecan against A-549, MCF-7, and LOVO cell lines. Moreover, compound 14c shows potent tumour inhibitory activity in a Colo205 xenograft model. [ABSTRACT FROM AUTHOR]