新型苯并[h]异喹啉衍生物的合成及生物学性质

Synthesis and biological properties of new benz[h]isoquinoline derivatives.

作者信息

Janin Y L, Carrez D, Riou J F, Bisagni E

机构信息

URA 1387 CNRS, Institut Curie Section de Biologie, Centre Universitaire, Orsay, France.

出版信息

Chem Pharm Bull (Tokyo). 1994 Apr;42(4):892-5. doi: 10.1248/cpb.42.892.

DOI:10.1248/cpb.42.892

Abstract

In order to determine the importance of the pyrrolic nitrogen atom in a series of suitably substituted gamma-carbolines derivatives for their cytotoxic and antitumor properties, a series of structurally related benz[h]isoquinolines were synthesized. When compared to the "parent" gamma-carbolines, these new compounds showed greatly decreased effects on topoisomerases I and II. Whereas the 8-hydroxylated derivatives retained a significant cytotoxicity, all the new compounds were devoid of antitumor effect in the P388 murine ip-ip system.

摘要

为了确定一系列适当取代的γ-咔啉衍生物中吡咯氮原子对其细胞毒性和抗肿瘤特性的重要性，合成了一系列结构相关的苯并[h]异喹啉。与“母体”γ-咔啉相比，这些新化合物对拓扑异构酶I和II的作用大大降低。虽然8-羟基化衍生物保留了显著的细胞毒性，但所有新化合物在P388小鼠腹腔注射-腹腔注射系统中均无抗肿瘤作用。

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