7-Substituted camptothecin derivatives

Abstract

Abstract New 7-substituted camptothecin derivatives possessing anti-tumor activity with slight toxicity, represented by the general formula: ##STR1## wherein R stands for --CHO, --CH 2 OR', --CH(OR') 2 or --CH═N--X where R' is a lower alkyl group with 1-6 carbon atoms or a phenylalkyl group with 1-3 carbon atoms in the alkylene moiety thereof, and X is a hydroxyl group or --NR 1 R 2 where R 1 and R 2 are the same or different and each represents a hydrogen atom or a lower alkyl group with 1-6 carbon atoms, or when R 1 is hydrogen, R 2 may be a lower alkyl group with 1-6 carbon atoms, a substituted or unsubstituted aryl group, a carbamoyl group, an acyl group, an aminoalkyl group or an amidino group, or when R 1 is the lower alkyl group, R 2 may be an aminoalkyl group, or R 1 and R 2 may be combined together with the nitrogen atom, to which R 1 and R 2 are bound, to form a heterocyclic group, and quaternary salts thereof. These 7-substituted camptothecin derivatives are prepared by treating 7-hydroxymethyl- or 7-dialkoxymethyl-camptothecin with a catinoid reagent, or treating 7-formyl- or 7-hydroxymethyl-camptothecin with an acid in the presence of a lower alkanol or phenylalkanol, or treating 7-formylcamptothecin or an acetal thereof with a nitrogen-containing carbonyl reagent and optionally treating the resulting product with a quaternating agent.

Inventors

• 👤 Tadashi Miyasaka
• 👤 Masahiko Mutai
• 👤 Seigo Sawada
• 👤 Kenichiro Nokata

Bibliographic Details