K. Swapna, N. Satheesh Kumar, N. Malla Reddy, M. Ravinder
{"title":"作为表皮生长因子受体靶向药物的新型喹啉-噻唑烷-2,4-二酮-异恶唑共轭物的设计与合成","authors":"K. Swapna, N. Satheesh Kumar, N. Malla Reddy, M. Ravinder","doi":"10.1134/S1070363224070193","DOIUrl":null,"url":null,"abstract":"<p>A series of new quinoline-thiazolidine-2,4-dione-isoxazole conjugates was synthesized and evaluated for <i>in vitro</i> anticancer potency against two breast cancer cell lines, such as MCF-7, MDA-MB231, and the normal cancer cell line MCF-10 A (breast cell line) using erlotinib as a standard drug. (<i>Z</i>)-3-{[5-(4-Methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione and (<i>Z</i>)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione showed higher anticancer activities against two cancer cell lines, with IC<sub>50</sub> ranging from 3.10 ± 0.43, 2.01 ± 0.03, 3.04 ± 0.05, and 2.00 ± 0.07 μM. Furthermore, (<i>Z</i>)-3-{[5-(4-methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione, and (<i>Z</i>)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione displayed more inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"94 7","pages":"1758 - 1767"},"PeriodicalIF":0.9000,"publicationDate":"2024-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design and Synthesis of Some New Quinoline-thiazolidine-2,4-dione-isoxazole Conjugates as EGFR Targeting Agents\",\"authors\":\"K. Swapna, N. Satheesh Kumar, N. Malla Reddy, M. Ravinder\",\"doi\":\"10.1134/S1070363224070193\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>A series of new quinoline-thiazolidine-2,4-dione-isoxazole conjugates was synthesized and evaluated for <i>in vitro</i> anticancer potency against two breast cancer cell lines, such as MCF-7, MDA-MB231, and the normal cancer cell line MCF-10 A (breast cell line) using erlotinib as a standard drug. (<i>Z</i>)-3-{[5-(4-Methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione and (<i>Z</i>)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione showed higher anticancer activities against two cancer cell lines, with IC<sub>50</sub> ranging from 3.10 ± 0.43, 2.01 ± 0.03, 3.04 ± 0.05, and 2.00 ± 0.07 μM. Furthermore, (<i>Z</i>)-3-{[5-(4-methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione, and (<i>Z</i>)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione displayed more inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.</p>\",\"PeriodicalId\":761,\"journal\":{\"name\":\"Russian Journal of General Chemistry\",\"volume\":\"94 7\",\"pages\":\"1758 - 1767\"},\"PeriodicalIF\":0.9000,\"publicationDate\":\"2024-08-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Russian Journal of General Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1134/S1070363224070193\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of General Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1070363224070193","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Design and Synthesis of Some New Quinoline-thiazolidine-2,4-dione-isoxazole Conjugates as EGFR Targeting Agents
A series of new quinoline-thiazolidine-2,4-dione-isoxazole conjugates was synthesized and evaluated for in vitro anticancer potency against two breast cancer cell lines, such as MCF-7, MDA-MB231, and the normal cancer cell line MCF-10 A (breast cell line) using erlotinib as a standard drug. (Z)-3-{[5-(4-Methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione and (Z)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione showed higher anticancer activities against two cancer cell lines, with IC50 ranging from 3.10 ± 0.43, 2.01 ± 0.03, 3.04 ± 0.05, and 2.00 ± 0.07 μM. Furthermore, (Z)-3-{[5-(4-methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione, and (Z)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione displayed more inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.
期刊介绍：
Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.
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