Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Molecules. 2013 Feb 26;18(3):2518-27. doi: 10.3390/molecules18032518.
A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
一系列取代的乙基 1-[(叔丁氧基羰基)氨基]-2-甲基-5-（1-甲基-1H-吲哚-3-基）-4-[(1-甲基-1H-吲哚-3-基）羰基]-1H-吡咯-3-羧酸酯通过β-二羰基化合物 12a-e 和 1,2-二氮杂-1,3-二烯（DD）13 的一锅反应以极好的产率（82-98%）制备。衍生物 10a，c-e，是双吲哚生物碱托品碱的去氮类似物，经美国国立癌症研究所（马里兰州贝塞斯达）在体外一次剂量针对约 60 个人类肿瘤细胞系的原发性抗癌测定中筛选，除了化合物 9e 外，没有显示出显著的活性，化合物 9e 对非小细胞肺癌亚组的 HOP-92 细胞系和中枢神经系统亚组的 SNB-75 细胞系具有中等活性。
