Novel anthracycline derivatives containing...

C - Chemistry – Metallurgy – 07 – H

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C07H 15/252 (2006.01) A61K 31/70 (2006.01) C07C 31/42 (2006.01) C07C 43/178 (2006.01) C07H 5/02 (2006.01) C07H 13/02 (2006.01) C07H 13/04 (2006.01) C07H 15/18 (2006.01)

Patent

CA 2185247

Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): Image (I) wherein R is a hydrogen atom or a hydroxyl group, and 7-O-(2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)- adriamycinone derivative which is an adriamycinone derivative represented by formula (II): Image (II) have now been newly synthesized. The novel anthracycline derivatives having the general formula (I) and formula (II), respectively, show excellent anticancer or antitumor activities and are of low toxicities. These novel compounds are very useful as anticancer or antitumor agents and are expected to be useful for the therapeutic treatments of a variety of cancers and tumors, similarly to daunomycin or adriamycin.

Nouveaux dérivés d'anthracycline représentés par les formules générales (I) et (II), présentant une activité antitumorale supérieure à celle des antibiotiques utilisés couramment comme cancérostatiques, tels que la daunomycine et l'adriamycine, ainsi qu'une faible toxicité. Dans ladite formule (I) R représente l'hydrogène ou un hydroxyle.

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