新型稠合菲咯啉的设计、合成、分子模拟及抗癌活性研究。
Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines.
机构信息
Faculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, Iasi 700506, Romania.
出版信息
Molecules. 2020 Jan 25;25(3):527. doi: 10.3390/molecules25030527.
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 and ) 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 showed a broad spectrum in terms of antiproliferative efficacy with GI values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds and are accommodated in the colchicine binding site of tubulin in two different ways.
设计了三个系列的稠合吡咯并菲咯啉衍生物作为苯并菲斯汀的类似物，分别以 1,7-菲咯啉、4,7-菲咯啉和 1,10-菲咯啉为起始原料，经两步法合成。在所测试的四种化合物中，有两种（化合物 和 ）对国立癌症研究所（NCI）的六十个人类癌细胞系进行了测试，对几种细胞系表现出显著的生长抑制活性。化合物 在抗增殖功效方面表现出广谱性，GI 值范围为 0.296 至 250 μM。分子对接研究表明，化合物 和 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。
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