2,9-Dimethyl-1,10-phenanthroline (2,9-DMP), a copper-specific chelator, was a potent cytotoxin against L1210 cells in vitro; its activity was dependent upon available Cu2+ in the medium. Other divalent ions, Fe2+ and Zn2+, were ineffective as promoters of growth inhibition. As the copper chelate, a 4 microM solution produced a 4 log kill after a 1-hr incubation. This was in marked contrast to 1,10-phenanthroline, whose inhibition of cell growth was overcome by added Cu2+, Fe2+ and Zn2+. Cellular uptake of labeled 2,9-dimethyl-1,10-phenanthroline also required added Cu2+ in the medium. This transport was energy dependent, and the drug was concentrated over 200-fold by the cells. In preliminary evaluations, copper-2,9-DMP showed significant chemotherapeutic activity against the P388 murine lymphoma in vivo.

中文翻译：

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2,9-二甲基-1,10-菲咯啉（新鸟嘌呤）：一种有效的铜依赖性细胞毒素，具有抗肿瘤活性。

2,9-二甲基-1,10-菲咯啉（2,9-DMP）是一种铜特异性螯合剂，在体外是针对L1210细胞的有效细胞毒素。它的活性取决于培养基中可用的Cu2 +。其他二价离子Fe2 +和Zn2 +不能有效地促进生长。作为铜螯合物，在孵育1小时后，4 microM溶液产生了4 log的杀灭。这与1,10-菲咯啉形成鲜明对比，后者通过添加Cu2 +，Fe2 +和Zn2 +克服了对细胞生长的抑制作用。标记的2,9-二甲基-1,10-菲咯啉的细胞摄取也需要在培养基中添加Cu2 +。这种转运是能量依赖性的，药物被细胞浓缩了200倍以上。在初步评估中，铜2,9-DMP在体内对P388鼠淋巴瘤显示出显着的化学治疗活性。