Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms of antiproliferative efficacy with GI50 values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds 8a and 11c are accommodated in the colchicine binding site of tubulin in two different ways.

中文翻译：

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新型稠合菲咯啉的设计、合成、分子建模和抗癌活性

三个系列的稠合吡咯并菲咯啉衍生物被设计为非他汀的类似物，并分两步合成，分别从 1,7-菲咯啉、4,7-菲咯啉和 1,10-菲咯啉开始。四种化合物中的两种（化合物 8a 和 11c）针对美国国家癌症研究所 (NCI) 的一组 60 种人类癌细胞系进行测试，对几种细胞系表现出显着的生长抑制活性。化合物 11c 在抗增殖功效方面表现出广谱，GI50 值在 0.296 至 250 μM 的范围内。分子对接研究表明，化合物 8a 和 11c 以两种不同的方式容纳在微管蛋白的秋水仙碱结合位点中。