SYNTHESIS AND ANTITUMOR ACTIVITY OF 4'-O-ACYLANTHRACYCLINES

SHOHACHI NAKAJIMA; HIROYUKI KAWAI; NOBUYASU KOMESHIMA; MASAYUKI SAKAKIBARA; KUNIAKI TATSUTA; NOBORU OTAKE; HAMAO UMEZAWA

doi:10.7164/antibiotics.45.374

SHOHACHI NAKAJIMA, HIROYUKI KAWAI, NOBUYASU KOMESHIMA, MASAYUKI SAKAKIBARA, KUNIAKI TATSUTA, NOBORU OTAKE, HAMAO UMEZAWA

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JOURNAL FREE ACCESS

1992 Volume 45 Issue 3 Pages 374-379

DOI https://doi.org/10.7164/antibiotics.45.374

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Abstract

4'-O-Acyl derivatives of doxorubicin, daunorubicin, 13-deoxocarminomycin, 13-deoxo-10-hydroxycarminomycin, 13-deoxo-ll-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.

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