Department of Organic Chemistry, University of Chemical Technology and Metallurgy, 8, Saint Kliment Ohridski Blvd., Sofia 1756, Bulgaria.
Eur J Med Chem. 2011 Jun;46(6):1992-6. doi: 10.1016/j.ejmech.2011.02.018. Epub 2011 Mar 3.
Novel molecular complexes of 1,10-phenanthroline (phen) and 5-amino-1,10-phenanthroline (5-NH2-phen) [(5-NH2-phen)2(phen) (H2O)3 (1), (phen)2(imidazole) (H+) (BF4-) (2), (phen)2(benzimidazole) (H+) (BF4-) (3), (5-NH2-phen)4(H2O)3 (4), and (phen)3 (indole) (H+) (BF4-) (5)] were synthesized via self-assembly processes and their in vitro anticancer activity was investigated. The structures of the compounds were confirmed by UV, FTIR, CIMS(CH4) and elemental analysis. The crystal structure of 2 was determined by X-ray diffraction. Cytotoxicity of the substances was measured using the cultivated human tumour cell lines HepG2, HEp-2, and 8-MB-GA. The tested substances showed different activity depending on the cell line and amount used. Substances 2 and 3 were not toxic to the non-tumour cells (Lep-3), but significantly toxic to all tumour ones. This is not the case with compounds 4 and 5, which are non-toxic towards carcinogenic cell lines, but even stimulate both HepG2 and HEp-2.
通过自组装过程合成了 1,10-菲咯啉（phen）和 5-氨基-1,10-菲咯啉（5-NH2-phen）的新型分子配合物[(5-NH2-phen)2(phen) (H2O)3 (1), (phen)2(imidazole) (H+) (BF4-) (2), (phen)2(benzimidazole) (H+) (BF4-) (3), (5-NH2-phen)4(H2O)3 (4), and (phen)3 (indole) (H+) (BF4-) (5)]，并研究了它们的体外抗癌活性。通过紫外、红外、CIMS(CH4)和元素分析确认了化合物的结构。通过 X 射线衍射确定了 2 的晶体结构。用培养的人肿瘤细胞系 HepG2、HEp-2 和 8-MB-GA 测量了物质的细胞毒性。测试物质的活性因细胞系和用量而异。物质 2 和 3 对非肿瘤细胞（Lep-3）没有毒性，但对所有肿瘤细胞都有明显的毒性。化合物 4 和 5 则不然，它们对致癌细胞系没有毒性，但对 HepG2 和 HEp-2 都有刺激作用。
