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4-Demethoxy-3'-N-trifluoroacetyldoxorubicin. Synthesis and solid tumor activity
D Horton1, W Priebe, J P Carter
1Department of Chemistry, Ohio State University, Columbus 43210.
Drug Design and Delivery
|June 1, 1990
Abstract:
A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and by 52% when it was given orally at 50 mg/kg.