首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Synthesis and preliminary evaluation activity studies of novel 4-(aryl/heteroaryl-2-ylmethyl)-6-phenyl-2-[3-(4-substituted-piperazine-1-yl)propyl]pyridazin-3(2H)-one derivatives as anticancer agents
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Synthesis and preliminary evaluation activity studies of novel 4-(aryl/heteroaryl-2-ylmethyl)-6-phenyl-2-[3-(4-substituted-piperazine-1-yl)propyl]pyridazin-3(2H)-one derivatives as anticancer agents

机译:新型4-(芳基/杂芳基-2-基甲基)-6-苯基-2- [3-(4-取代-哌嗪-1-基)丙基]哒嗪-3(2H)-的合成及初步评价活性衍生物作为抗癌药

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摘要

A series of new 4-(aryl/heteroaryl-2-ylmethyl)-6-phenyl-2-[3-(4-substituted piperazine-1-yl)propyl] pyri-dazin-3(2H)-one derivatives were synthesized. The structures of the compounds were confirmed by IR, ~1H NMR, and mass spectral data. All the compounds were evaluated for their cytotoxicity toward five human cancer cell lines of different origins viz; HeLa (Cervical), SKBR3 (Breast), HCT116 (Colon), A375 (Skin) & H1299 (Lung) at different concentrations and the IC_(50) values were determined. HCT116 and HeLa are the most sensitive against the compounds studied. One of them displayed moderate cytotoxicity against SKBR3. Majority of the compounds exhibited good to moderate activity.
机译:合成了一系列新的4-(芳基/杂芳基-2-基甲基)-6-苯基-2- [3-(4-取代的哌嗪-1-基)丙基]哒嗪-3(2H)-衍生物。化合物的结构通过IR,〜1H NMR和质谱数据证实。评估了所有化合物对五种不同来源的人类癌细胞系的细胞毒性。 HeLa(宫颈),SKBR3(乳腺癌),HCT116(结肠),A375(皮肤)和H1299(肺)处于不同浓度,并确定了IC_(50)值。 HCT116和HeLa对研究的化合物最敏感。其中之一显示出对SKBR3的中等细胞毒性。大多数化合物表现出良好至中等的活性。

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