Glutathione derivatives of anthracyclines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514562, 549358, 552201, 562427, C07D31904, C07D31908, C07D 5022

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active

056461771

ABSTRACT:
Disclosed herein are new anthracyclines which are derived from conjugation with glutathione, for example from conjugation of adriamycin, daunomycin and menogaril with glutathione: compounds 7 I, 7 II, 8 I, 8 II, 9 I and 9II, are obtained by reduction of the anthracycline followed by reaction of the reduced product with glutathione in aqueous (H.sub.2 O or D.sub.2 O) or organic solvent. The invention also provides salts of these glutathione derivatives, particularly salts formed from anthracycline glutathione anions with anthracycline cations. These anthracycline derivatives are useful as antibiotics, as antitumor agents, and in the treatment of AIDS. These derivatives are particularly useful in the treatment of cancer when multiple drug resistance is present.

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