Improved Antitumor Activity by Modification of Nogalamycin

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Abstract
Nogalamycin, an antitumor antibiotic, was converted to a series of analogs by removal of the carbomethoxy group at C-10 and replacement of the neutral sugar at C-7 by other groups. Removal of the carbomethoxy group to given disnogamycin (6) followed by acidic alcoholysis gave pairs of isomeric 7-alkoxy compounds differing in configuration at C-7. Treatment of 6 with trifluoroacetic acid followed by nucleophiles gave a series of analogs having substituents at C-7 with a configuration at C-7 opposite to that of nogalamycin. Among the analogs prepared, 7-con-O-methylnogarol (7) was a highly active antitumor agent [when tested against murine leukemia P-388 and L-1210 cells and mouse melanoma B16 cells].

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