Synthesis and in vitro anticancer activity of some novel tetrahydroquinoline derivatives bearing pyrazol and hydrazide moiety,Journal of Heterocyclic Chemistry

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Synthesis and in vitro anticancer activity of some novel tetrahydroquinoline derivatives bearing pyrazol and hydrazide moiety
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-02-24 , DOI: 10.1002/jhet.3930
Usama Fathy ₁ , Mariam A. Azzam ₁ , Fathia Mahdy ₁ , Somia El‐Maghraby ₁ , Rasha M. Allam ₂

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A new series of tetrahydroquinoline derivatives having pyrazol and hydrazide moieties were synthesized for the purpose of anticancer cell line evaluation. Syntheses of these compounds were firstly achieved by one pot four reactions. The reaction of 3‐amino‐tetrahydro‐1H‐pyrazolo [3,4‐b]quinolin with aldehydes, indoline‐2,3‐dione derivatives to give 9a‐c, 11a‐c, and 13a,b, respectively. In similar manner for biological comparison, the reactions of compound 5 with the same aldehydes and indoline‐2,3‐dione derivatives to give 19a‐c and 20a‐c. The newly synthesized compounds were examined in vitro for their cytotoxic activity against HepG‐2 and A549 cancer cells. The compounds 11a‐c and 20a‐c showed promising activity as anticancer agents against HepG‐2 and A549 cancer cells.

中文翻译：

一些带有吡唑和酰肼部分的新型四氢喹啉衍生物的合成及其体外抗癌活性

为了评估抗癌细胞系，合成了具有吡唑和酰肼部分的一系列新的四氢喹啉衍生物。这些化合物的合成首先通过一锅四反应来实现。3-氨基四氢-1 H-吡唑并[3,4-b]喹啉与醛，二氢吲哚-2-3-二酮衍生物的反应，分别得到9a-c，11a-c和13a，b。以类似的方式进行生物学比较，化合物5与相同的醛和二氢吲哚-2,3-二酮衍生物反应生成19a-c和20a-c。在体外检查了新合成的化合物对HepG-2和A549癌细胞的细胞毒活性。化合物11a-c和20a-c显示出有希望的抗HepG-2和A549癌细胞活性。

更新日期：2020-02-24

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