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Abstract：
Newly synthesized 7-chloro-4-aminoquinoline-benzimidazole hybrids were characterized by NMR and elemental analysis. Compounds were tested for their effects on the growth of the non-tumor cell line MRC-5 (human fetal lung fibroblasts) and carcinoma (HeLa and CaCo-2), leukemia, and lymphoma (Hut78, THP-1, and HL-60) cell lines. The obtained results, expressed as the concentration at which 50% inhibition of cell growth is achieved (IC50 value), show that the tested compounds affect cell growth differently depending on the cell line and the applied dose (IC50 ranged from 0.2 to >100 µM). Also, the antiplasmodial activity of these hybrids was evaluated against two P. falciparum strains (Pf3D7 and PfDd2). The tested compounds showed potent antiplasmodial activity, against both strains, at nanomolar concentrations. Quantitative structure-activity relationship (QSAR) analysis resulted in predictive models for antiplasmodial activity against the 3D7 strain (R2 = 0.886; Rext2 = 0.937; F = 41.589) and Dd2 strain (R2 = 0.859; Rext2 = 0.878; F = 32.525) of P. falciparum. QSAR models identified the structural features of these favorable effects on antiplasmodial activities.
摘要：
新合成的7-氯-4-氨基喹啉-苯并咪唑杂化物通过NMR和元素分析进行了表征。测试了化合物对非肿瘤细胞系MRC-5（人胎儿肺成纤维细胞）和癌（HeLa和CaCo-2）的生长的影响，白血病,和淋巴瘤（Hut78，THP-1和HL-60）细胞系。所获得的结果,表示为达到50%细胞生长抑制的浓度（IC50值），显示受试化合物影响细胞生长不同，取决于细胞系和应用剂量（IC50范围为0.2至>100µM）。此外，针对两种恶性疟原虫菌株(Pf3D7和PfDd2)评估了这些杂种的抗疟原虫活性。测试的化合物显示出有效的抗疟原虫活性，对抗这两种菌株，在纳摩尔浓度。定量结构-活性关系(QSAR)分析产生了针对恶性疟原虫的3D7菌株(R2=0.886;Rext2=0.937;F=41.589)和Dd2菌株(R2=0.859;Rext2=0.878;F=32.525)的抗疟原虫活性的预测模型。QSAR模型确定了这些对疟原虫活性有利作用的结构特征。
