Synthesis and antitumor activity of 4-demethoxydaunorubicin, 4-demethoxy-7,9-diepidaunorubicin, and their beta anomers
Arcamone, F.; Bernardi, L.; Giardino, P.; Patelli, B.; Marco, A.; Casazza, A.M.; Pratesi, G.; Reggiani, P.
Cancer Treatment Reports 60(7): 829-834
1976
ISSN/ISBN: 0361-5960 PMID: 1009518 Document Number: 108688
Four new derivatives of daunorubicin, characterized by the absence of the methoxyl group at the C-4 position, have been obtained by chemical synthesis. 4-Demethoxydaunorubicin (NSC-256439) was effective against L1210 and Gross leukemias and ascites and solid Sarcoma 180 at doses four to eight times lower than those effective for daunorubicin. The beta anomer of 4-demethoxydaunorubicin was active at doses 13and eight times higher than those of its corresponding alpha anomer against L1210 and Gross leukemias respectively. 4-Demethoxy-7,9-diepidaunorubicin and its beta anomer were devoid of any biologic activity at the doses tested.