DITERPENE ALKALOID DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS THEREOF

摘要

The invention relates to a novel Raspailia sp. to cytotoxic alkaloids of general formula (I) and (II) isolated from sponge, including asmarin A and B. The structures of the compounds were determined from NMR data and confirmed by X-ray analysis. In the compounds of formulas (I) and (II) according to the invention, R1 represents a hydrogen atom or an alkyl or alkanoyl group; R2 is hydrogen or alkyl; R3 is an alkyl or cycloalkyl group containing one or more isoprene units, or a monoterpene or sesquiterpene or diterpene group; R4 and R5 are hydrogen or alkyl; R6 is alkyl and X is fluoro, chloro, bromo or iodo. The present invention relates to a process for the preparation of the above compounds, to the use of the compounds for the preparation of pharmaceutical compositions having antitumor activity, and to pharmaceutical compositions containing the compounds. SHE