A Convenient Synthesis and Biological Research of Novel 5,6,7,8‐Tetrahydro‐1,6‐naphthyridin‐2(1H)‐one Derivatives Hydrochloride as Cytotoxic Agents,Journal of Heterocyclic Chemistry

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A Convenient Synthesis and Biological Research of Novel 5,6,7,8‐Tetrahydro‐1,6‐naphthyridin‐2(1H)‐one Derivatives Hydrochloride as Cytotoxic Agents
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2018-07-13 , DOI: 10.1002/jhet.3273
Guiqing Xu ₁ , Yuan Gao ₁ , Bin Sun ₂ , Lizeng Peng ₃ , Longfei Mao ₁ , Yuqin Jiang ₁ , Qingjie Ding ₁

Affiliation

A series of 5,6,7,8‐tetrahydro‐1,6‐naphthyridin‐2(1H)‐one derivatives hydrochloride were obtained using a convenient and mild method from 4‐piperidone monohydrate hydrochloride. The newly synthesized compounds and their derivatives were characterized by ¹H NMR, ¹³C NMR, and high‐resolution mass spectrometry. Furthermore, cytotoxicity in vitro of the synthesized compounds were screened using MTT or CCK8 assay. The results showed that some of the compounds showed potential antitumor activity. Among of them, compound 10a had effects against tumor cells (MOLM‐13), and the half maximal inhibitory concentration value was 76 μmol/L.

中文翻译：

新型5,6,7,8-四氢-1,6-萘啶-2-2（1H）-1衍生物盐酸盐作为细胞毒剂的简便合成及生物学研究

使用方便和温和的方法从4-哌啶酮一水合物盐酸盐中获得了一系列5,6,7,8-四氢-1,6-萘啶2-2（1 H）-one盐酸盐。通过¹ H NMR，¹³ C NMR和高分辨率质谱对新合成的化合物及其衍生物进行了表征。此外，使用MTT或CCK8测定法筛选了合成化合物的体外细胞毒性。结果表明，某些化合物具有潜在的抗肿瘤活性。其中，化合物10a对肿瘤细胞（MOLM-13）有作用，最大抑制浓度值的一半为76μmol/ L。

更新日期：2018-07-13

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