An expedient multi‐component synthesis of pyridinyl‐spirooxindoles and their effect on proliferation of lung cancer A549 cells,Journal of Heterocyclic Chemistry

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An expedient multi‐component synthesis of pyridinyl‐spirooxindoles and their effect on proliferation of lung cancer A549 cells
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-08-03 , DOI: 10.1002/jhet.4114
Liang Yan ₁ , Xu Wu ₁ , Yizongheng Zhang ₂ , Mathan Sankaran ₃ , Lei Xu ₁ , Liefeng Ling ₁ , Yi Wang ₃ , Yuxin Jiang ₄ , Jinzhu Ma ₁ , Lingyu Kong ₃

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A series of new functionalized pyridinyl‐spirooxindoles have been synthesized through three‐component cyclization reactions. The selected compounds were screened for their in vitro antiproliferative activity against human lung cancer cell line A549. Among the candidate structures, compound 1o demonstrated maximum inhibitory activity against A549 cells with IC₅₀ values of 28.38 μM. EdU (5‐Ethynyl‐2′‐ deoxyuridine, EdU) assay and cell colony formation test showed that cell proliferation of A549 cells was inhibited. In addition, Western blot analysis revealed that the phosphorylation levels of Akt, mTOR, 70S6, and S6 were down‐regulated. Thus, these results indicated that 1o may inhibit the proliferation of A549 cells through inhibiting the phosphorylation levels of Akt, mTOR, 70S6, and S6. 1o may be developed as a potential antitumor agent for lung cancer treatment.

中文翻译：

吡啶基-螺硫辛多酯的简便多组分合成及其对肺癌A549细胞增殖的影响

通过三组分环化反应，已经合成了一系列新型的官能化吡啶基-螺并氧杂吲哚。筛选所选择的化合物对人肺癌细胞系A549的体外抗增殖活性。在候选结构中，化合物1o表现出对A549细胞的最大抑制活性，IC ₅₀值为28.38μM。EdU（5-乙炔基-2'-脱氧尿苷，EdU）检测和细胞集落形成测试表明，A549细胞的细胞增殖受到抑制。此外，蛋白质印迹分析表明Akt，mTOR，70S6和S6的磷酸化水平被下调。因此，这些结果表明1o可能通过抑制Akt，mTOR，70S6和S6的磷酸化水平来抑制A549细胞的增殖。1o可能被开发为潜在的抗肺癌药物。

更新日期：2020-08-03

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