Camptothecin-1-oxide derivatives, process for preparing same, formulations comprising said derivatives and said derivatives for use in producing an anti-tumour effect

摘要

New 5- and/or 7-substituted camptothecin-1-oxide derivatives possessing anti-tumor activity with slight toxicity are represented by the general formula:wherein R is a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group, and R' is a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, an acloxymethyl group or a carboxymethyl group, with the proviso that R and R' are not both hydrogen atoms. These 5- and/or 7-substituted camptothecin-1-oxide derivatives may be prepared by treating the corresponding 5- and/or 7-substituted camptothecins with a peroxidant as an N-oxidizing reagent.