苯并噻唑衍生物合成的噻吩、噻唑和吡嗪衍生物的细胞毒活性和形态研究[d]

IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Acta Chimica Slovenica Pub Date : 2023-09-20 DOI:10.17344/acsi.2023.8057
Karam Ahmed El-Sharkawy, Rafat Milad Mohareb, Sayeed Mukhtar, Humaira Parveen, Mahmoud Ali Abdelaziz
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引用次数: 0

摘要

合成了苯并[d]噻唑衍生物4a-c,并用于合成噻吩衍生物6a-f。它们形成芳基腙衍生物8a-i,而8a-i又能形成吡嗪衍生物9a-i和10a-i。后两种化合物分别与巯基乙酸反应生成噻唑衍生物12a-i和13a-i。以4a-c为原料,与单质硫和苯异硫氰酸酯反应,得到了噻唑衍生物15a-c。进一步对15a进行杂环化反应,得到噻吩衍生物。对合成的产物进行了针对一些选定的癌细胞系的评价,并对根据疾病分类的17种癌细胞系进行了最有效的化合物进一步评价。利用肺组织微环境研究了化合物13c和13h对A549细胞系形态学的影响,获得了良好的结果。
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Cytotoxic Activities and Morphological Sudies of Thiophene, Thiazole and Pyridazine Derivatives Synthesized from Benzo[d]thiazole Derivatives
The benzo[d]thiazole derivatives 4a–c were synthesized and used for the synthesis of thiophene derivatives 6a–f. They form the arylhydrazone derivatives 8a–i which were capable to form pyridazine derivatives 9a–i and 10a–i. The latter compounds reacted with thioglycolic acid to produce the thiazole derivatives 12a–i and 13a–i, respectively. The thiazole derivatives 15a–c were also produced from 4a–c through their reactions with elemental sulfur and phenylisothiocyanate. Further heterocyclization reactions of 15a were carried out to produce thiophene derivatives. Evaluations of the synthesized products were carried out against some selected cancer cell lines and the most active compounds were further evaluated against the seventeen cancer cell lines classified according to the disease. Morphological changes of A549 cell line by the effect of compounds 13c and 13h were studied using microenvironment of the lung tissue where an excellent result was obtained.
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来源期刊
Acta Chimica Slovenica
Acta Chimica Slovenica 化学-化学综合
CiteScore
2.50
自引率
25.00%
发文量
80
审稿时长
1.0 months
期刊介绍: Is an international, peer-reviewed and Open Access journal. It provides a forum for the publication of original scientific research in all fields of chemistry and closely related areas. Reviews, feature, scientific and technical articles, and short communications are welcome.
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