Document Report Card

ID: ALA1126683

Journal: J Med Chem

Title: Synthesis and antitumor activity of isodoxorubicin analogues.

Authors: Florent JC, Gaudel G, Monneret C, Hoffmann D, Kraemer HP.

Abstract: The synthesis and biological activity of the new 4-demethoxyanthracyclines 15, 22, and 23 are reported. They were obtained from synthetic 9-deacetyl-9-(hydroxymethyl)-4-demethoxydaunomycinone (isopropylidene derivative 9) and from 4-azido- or 4-amino-2,4,6-trideoxy-L- lyxo-hexoses. Anthracycline 22 (hydrochloride salt), the most active compound in the series, was slightly more potent than doxorubicin in vitro against three cell lines (L1210, HT29, A549). It was found to exhibit similar antitumor activity in vivo (iv route) against L1210 leukemia, but was less active than doxorubicin against three human tumors in a subrenal capsule assay LXF, A549, and HT29).

CiteXplore: 8496904

DOI: 10.1021/jm00062a008