> Incorporation of heterocyclic pyrimidine or pyridine motifs is common in the drug design for various therapeutic applications. Herein, we descr'/> Pyrimidine Derivatives with Terminal Pyridyl Heterocycles: Facile Synthesis and Their Antiproliferative Activities
首页> 外文期刊>Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry >Pyrimidine Derivatives with Terminal Pyridyl Heterocycles: Facile Synthesis and Their Antiproliferative Activities
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Pyrimidine Derivatives with Terminal Pyridyl Heterocycles: Facile Synthesis and Their Antiproliferative Activities

机译:嘧啶衍生物与末端吡啶基杂环:容易合成及其抗增殖活动

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摘要

> Incorporation of heterocyclic pyrimidine or pyridine motifs is common in the drug design for various therapeutic applications. Herein, we describe the facile synthesis of two molecules containing both pyrimidine and pyridine scaffolds. A variety of analytical techniques (multinuclear NMR, Fourier transform infrared, and mass spectrometry analyses) confirmed the purity of these molecules. In pristine form, their potential as antitumor drugs was screened by investigating their cytotoxicity against various cell lines (cancerous and normal cells). Experimental results confirmed that the two molecules exhibited cell growth inhibition at very low concentrations. This was evident from their IC 50 values that are in the range of 0.45–2.20 μM.
机译:

杂环嘧啶或吡啶基序的掺入在各种治疗应用的药物设计中是常见的。 在此,我们描述了含有嘧啶和吡啶支架的两种分子的容易合成。 各种分析技术(多核NMR,傅里叶变换红外和质谱分析)证实了这些分子的纯度。 以原始形式,通过针对各种细胞系(癌性和正常细胞)来筛选它们作为抗肿瘤药物的潜力。 实验结果证实,两种分子在非常低浓度下表现出细胞生长抑制。 这是从它们的IC 50 值中显而易见的,该值在0.45-2.20μm的范围内。

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