Florent J C, Gaudel G, Monneret C, Hoffmann D, Kraemer H P
Service de Chimie, CNRS, URA 1387, Institut Curie, Paris, France.
J Med Chem. 1993 May 14;36(10):1364-8. doi: 10.1021/jm00062a008.
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).
报道了新型4-去甲氧基蒽环类化合物15、22和23的合成及其生物活性。它们是由合成的9-脱乙酰基-9-(羟甲基)-4-去甲氧基柔红霉素酮（异丙叉衍生物9）与4-叠氮基-或4-氨基-2,4,6-三脱氧-L-来苏糖合成得到的。蒽环类化合物22（盐酸盐）是该系列中活性最强的化合物，在体外对三种细胞系（L1210、HT29、A549）的活性略强于阿霉素。发现在体内（静脉注射途径）对L1210白血病具有相似的抗肿瘤活性，但在肾包膜下试验中对三种人类肿瘤（LXF、A549和HT29）的活性低于阿霉素。
