Hydroxyindolones (1-6, 15-16) were transformed into isatinylidenes (7, 9-13, 17-19) by dehydration with 4-toluenesulfonic acid. The dimer-type compounds (14, 20) were also isolated in a few cases. The obtained isatinylidenes were transformed into 3-spiro-cyclopropane-oxindoles (21-32) with dimethyloxosulfonium methylide. Compound 22 shows protective effects against hypobaric hypoxia and triethyltin induced brain edema.
New Antitumor Hydroxymethyl Derivatives of Vinblastine. -New hydroxymethyl derivatives of the antitumor indole-indoline alkaloids vinblastine and leurosine are prepared by simple reduction of an ester group in the parent alkaloids [→ (II)] or by coupling of the monomer alkaloid catharanthine (VI) with vindoline derivatives [→ (VII)]. Among the new vinblastine derivatives, compound (II) shows highest cytotoxic activity. -(BOELCSKEI, H.; SZAN-TAY, C. JUN.; MAK, M.; BALAZS, M.; SZANTAY, C.; J. Indian Chem.
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