Synthesis and antitumor activity of 4'-O-acylanthracyclines.
4'-O-Acyl derivatives of doxorubicin, daunorubicin, 13-deoxocarminomycin, 13-deoxo-10-hydroxycarminomycin, 13-deoxo-11-deoxycarminomycin were synthesized through the formation and mild acid hydrolysis of 2-oxazoline intermediates. The antitumor activity of these 4'-O-acyl derivatives against P388 leukemia was similar to or more effective than the parent anthracyclines.
Nakajima
S
S
Pharmaceutical Laboratory, Kirin Brewery Co., Ltd., Gunma, Japan.
Kawai
H
H
Komeshima
N
N
Sakakibara
M
M
Tatsuta
K
K
Otake
N
N
Umezawa
H
H
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice
D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents