Faculty of Science, Department of Chemistry, Menoufia University, Shebin El-Koom, Egypt.
Biochemistry Division, Faculty of Science, Department of Chemistry, Menoufia University, Shebin El-Koom, Egypt.
Arch Pharm (Weinheim). 2018 May;351(5):e1700363. doi: 10.1002/ardp.201700363. Epub 2018 Apr 3.
A series of novel phthalimide analogs containing an indole or brominated indole moiety were synthesized and their antimicrobial activity was evaluated. Compound 8 showed a broad spectrum activity, revealing 53-67% of erythromycin activity on the tested bacteria and 60-70% of miconazole activity on the tested fungi. Anticancer activity was evaluated on the cell lines HepG2, MCF-7, A549, H1299, and Caco2. The results revealed that the new phthalimide analog 8 has broad-spectrum anticancer activity toward all the tested cancer cell lines, followed by compound 11, which showed good activity toward all the tested cell lines except for MCF-7. The ability of the promising analogs 5, 8, and 11 to bind to topoisomerase II DNA gyrase was investigated. Caspase-3 activation and Bcl-2 assay of the best active derivatives 8, 11 in addition to compound 5 were evaluated. The antifibrotic activity was studied in an in vivo model and the histopathological studies revealed that treatment with the new compound 8 improved the fibrotic liver tissues to normality.
一系列含有吲哚或溴代吲哚部分的新型邻苯二甲酰亚胺类似物被合成，并评估了它们的抗菌活性。化合物 8 表现出广谱活性，对测试的细菌显示出红霉素活性的 53-67%，对测试的真菌显示出咪康唑活性的 60-70%。在 HepG2、MCF-7、A549、H1299 和 Caco2 细胞系上评估了抗癌活性。结果表明，新型邻苯二甲酰亚胺类似物 8 对所有测试的癌细胞系均具有广谱抗癌活性，其次是化合物 11，它对除 MCF-7 之外的所有测试细胞系均表现出良好的活性。研究了有前途的类似物 5、8 和 11 与拓扑异构酶 II DNA 回旋酶结合的能力。评估了最佳活性衍生物 8、11 以及化合物 5 的 caspase-3 激活和 Bcl-2 测定。在体内模型中研究了抗纤维化活性，组织病理学研究表明，用新型化合物 8 治疗可改善纤维化的肝组织至正常状态。
