Nucleophile substituted ecteinascidins and n-oxide...

C - Chemistry – Metallurgy – 07 – D

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C07D 515/22 (2006.01) A61K 31/4985 (2006.01) A61P 35/00 (2006.01) C07D 241/36 (2006.01) C07D 237/26 (2006.01)

Patent

CA 2286796

Five new nucleophile substituted ecteinascidin (Et) compounds have been isolated from extracts of Ecteinascidia turbinata. These compounds have been purified by chromatographic techniques and their structures and bioactivities have been determined. The five nucleophile substituted Et compounds have been designated herein as Et 802 (1), Et 788 (2), Et 760 (3), Et 858 (4) and Et (815) (5). Also obtained were three new N-oxide ecteinascidin compounds, which have been designated herein as Et 717 (6), Et 775 (7) and Et 789 (8). Some of these newly discovered Et compounds show exceedingly potent cytotoxicity against L1210.

Cinq nouveaux composés d'ectéinascidine (Et) à substitution nucléophile ont été isolés d'extraits de Ecteniascidia turbinata. Ces composés ont été purifiés par des techniques chromatographiques, et leurs structures ainsi que leurs bioactivités ont été déterminées. Les cinq composés Et à substitution nucléophile ont été appelés ici Et 802 (1), Et 788 (2), Et 760 (3), Et 858 (4) et Et 815 (5). Trois nouveaux composés de N-oxyde ectéinascidine, qui ont été appelés ici Et 717 (6), Et 775 (7) et Et 789 (8) ont été également produits. Certains de ces nouveaux composés d'Et présentent une cytotoxicité extrêmement élevée à l'égard de L1210.

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