von Nussbaum F, Miller B, Wild S, Hilger C S, Schumann S, Zorbas H, Beck W, Steglich W
Institut für Organische Chemie der Universität München, Butenandtstrasse 5-13, D-81377 München, Germany.
J Med Chem. 1999 Sep 9;42(18):3478-85. doi: 10.1021/jm980434t.
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.
异喹啉广泛的生物学效应促使我们将其用作顺铂（II）抗肿瘤复合物中的螯合、非离去配体。本文报道了几种具有不同氢化水平和苯环不同取代基的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用于合成多环铂（II）复合物的新型配体。体外细胞毒性试验表明，碱性最强的胺配体形成的复合物最有效。两种新复合物对L1210小鼠白血病细胞的活性比成熟的抗肿瘤化合物顺铂更强。
