吲哚和氮杂吲哚与氧化二氢吡啶的新系列衍生物:针对乳腺恶性细胞系的合成、表征和细胞毒性研究

Q4 Chemistry
A. Madugula, K. Jagadeesh, D.B.N. Suresh Varma, K. G. Kadiyala, S. Pedada, Rama Swamy Guttula, U. Nagababu, Gururaja Rangaiah
{"title":"吲哚和氮杂吲哚与氧化二氢吡啶的新系列衍生物:针对乳腺恶性细胞系的合成、表征和细胞毒性研究","authors":"A. Madugula, K. Jagadeesh, D.B.N. Suresh Varma, K. G. Kadiyala, S. Pedada, Rama Swamy Guttula, U. Nagababu, Gururaja Rangaiah","doi":"10.14233/ajchem.2024.30317","DOIUrl":null,"url":null,"abstract":"In this investigation, a novel series of indole and azaindole comprising oxo-dihydropyridine derivatives was synthesized. From their spectral (1H NMR and FTIR) as well as elemental (MS) investigations, the structures of all the synthesized 12 oxo-dihydropyridine derivatives were determined. Cytotoxicity of synthesized twelve compound was evaluated against MDA-MB-231 malignant breast cells had been assessed. Compound 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed more percent of inhibition of growth and four more derivatives showed moderate percent of inhibition of growth counter to MDA-MB-231 malignant breast cells. The derivative 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed the highest effectiveness when assessing the IC50 value against the malignant breast cell line MDA-MB-231. Each of the compounds synthesized has a druggable character and meets Lipinski’s criteria of five.","PeriodicalId":8494,"journal":{"name":"Asian Journal of Chemistry","volume":"20 2","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A New Series of Indole and Azaindole Derivatives with Oxo-dihydropyridines: Synthesis, Characterization and Cytotoxicity Studies against Breast Malignant Cell Lines\",\"authors\":\"A. Madugula, K. Jagadeesh, D.B.N. Suresh Varma, K. G. Kadiyala, S. Pedada, Rama Swamy Guttula, U. Nagababu, Gururaja Rangaiah\",\"doi\":\"10.14233/ajchem.2024.30317\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"In this investigation, a novel series of indole and azaindole comprising oxo-dihydropyridine derivatives was synthesized. From their spectral (1H NMR and FTIR) as well as elemental (MS) investigations, the structures of all the synthesized 12 oxo-dihydropyridine derivatives were determined. Cytotoxicity of synthesized twelve compound was evaluated against MDA-MB-231 malignant breast cells had been assessed. Compound 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed more percent of inhibition of growth and four more derivatives showed moderate percent of inhibition of growth counter to MDA-MB-231 malignant breast cells. The derivative 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed the highest effectiveness when assessing the IC50 value against the malignant breast cell line MDA-MB-231. Each of the compounds synthesized has a druggable character and meets Lipinski’s criteria of five.\",\"PeriodicalId\":8494,\"journal\":{\"name\":\"Asian Journal of Chemistry\",\"volume\":\"20 2\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-02-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Asian Journal of Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.14233/ajchem.2024.30317\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"Chemistry\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Asian Journal of Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.14233/ajchem.2024.30317","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Chemistry","Score":null,"Total":0}
引用次数: 0

摘要

本研究合成了一系列新型吲哚和氮杂吲哚氧化二氢吡啶衍生物。通过光谱(1H NMR 和 FTIR)和元素(MS)分析,确定了合成的 12 种氧化二氢吡啶衍生物的结构。评估了合成的 12 种化合物对 MDA-MB-231 恶性乳腺细胞的细胞毒性。化合物 1,6-二氨基-4-(1H-吲哚-3-基)-2-氧代-1,2-二氢吡啶-3,5-二甲腈对 MDA-MB-231 恶性乳腺细胞的生长抑制率较高,另有四种衍生物对 MDA-MB-231 恶性乳腺细胞的生长抑制率中等。在评估对恶性乳腺细胞株 MDA-MB-231 的 IC50 值时,1,6-二氨基-4-(1H-吲哚-3-基)-2-氧代-1,2-二氢吡啶-3,5-二腈衍生物显示出最高的效力。合成的每个化合物都具有可药用特性,并符合利宾斯基的五项标准。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A New Series of Indole and Azaindole Derivatives with Oxo-dihydropyridines: Synthesis, Characterization and Cytotoxicity Studies against Breast Malignant Cell Lines
In this investigation, a novel series of indole and azaindole comprising oxo-dihydropyridine derivatives was synthesized. From their spectral (1H NMR and FTIR) as well as elemental (MS) investigations, the structures of all the synthesized 12 oxo-dihydropyridine derivatives were determined. Cytotoxicity of synthesized twelve compound was evaluated against MDA-MB-231 malignant breast cells had been assessed. Compound 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed more percent of inhibition of growth and four more derivatives showed moderate percent of inhibition of growth counter to MDA-MB-231 malignant breast cells. The derivative 1,6-diamino-4-(1H-indol-3-yl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile showed the highest effectiveness when assessing the IC50 value against the malignant breast cell line MDA-MB-231. Each of the compounds synthesized has a druggable character and meets Lipinski’s criteria of five.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Asian Journal of Chemistry
Asian Journal of Chemistry 化学-化学综合
CiteScore
0.80
自引率
0.00%
发文量
229
审稿时长
4 months
期刊介绍: Information not localized
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信