University of Colorado

The United States of America As Represented by the Department of Health

Consiglio Nazionale Delle Richerche

Giorgio Gaudiano

Tad H Koch

Steven D Averbuch

Nicholas R Bachur

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.

Glutathione derivatives of anthracyclines

The present invention discloses a bi(3,5-dimethyl-5-hydroxymethyl-2-oxomorpholin-3-yl) compound and its efficacy as a rescue agent against anthracycline and mitomycin C induced tissue damage. A method of synthesizing said compound has also been described.

Growing community of inventors

Boulder, CO, United States of America

Giorgio Gaudiano