Synthesis of 1-(2-aminophenyl)isoquinolines and the biological activity of their cis-dichloro platinum(II) complexes.
Synthesis of 1-(2-aminophenyl)isoquinolines and the biological activity of their cis-dichloro platinum(II) complexes.
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DOI：
10.1021/jm980434t
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发表时间：
1999-08
影响因子：
7.3
通讯作者：
F. von Nussbaum;B. Miller;S. Wild;C. Hilger;S. Schumann;H. Zorbas;W. Beck;W. Steglich
中科院分区：
文献类型：
--
作者：
F. von Nussbaum;B. Miller;S. Wild;C. Hilger;S. Schumann;H. Zorbas;W. Beck;W. Steglich
异喹啉类化合物广泛的生物学效应促使我们将其用作顺铂（II）抗肿瘤配合物中的螯合、非离去配体。报道了几种不同氢化程度和苯环取代度的1-（2-氨基苯基）异喹啉衍生物的合成。这些化合物构成了一类新的配体用于合成寡环铂（II）配合物。体外细胞毒性试验表明，最碱性的胺配体提供最有效的配合物。两个新的复合物对L1210小鼠白血病细胞比公认的抗肿瘤化合物顺铂更有效。
The broad biological effects of isoquinolines prompted us to use them as chelating, nonleaving ligands in cis-platinum(II) antitumor complexes. The synthesis of several 1-(2-aminophenyl)isoquinoline derivatives with different levels of hydrogenation and varying substitution of the phenyl ring is reported. These compounds constitute a new class of ligands for the synthesis of oligocyclic platinum(II) complexes. In vitro cytotoxicity tests indicate that the most basic amine ligands afford the most effective complexes. Two of the new complexes were more potent against L1210 murine leukemia cells than the well-established antitumor compound cisplatinum.