Synthesis of flavone-2'-carboxylic acid analogues as potential antitumor agents.

Anti-cancer drug design Pub Date : 1998-12-01
P Valenti, A Bisi, A Rampa, S Gobbi, F Belluti, P Da Re, L Cima, M Carrara
{"title":"Synthesis of flavone-2'-carboxylic acid analogues as potential antitumor agents.","authors":"P Valenti,&nbsp;A Bisi,&nbsp;A Rampa,&nbsp;S Gobbi,&nbsp;F Belluti,&nbsp;P Da Re,&nbsp;L Cima,&nbsp;M Carrara","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>Some flavone-2'-carboxylic acid analogues are described. Direct in vitro toxicity of the synthesized compounds was evaluated towards four tumoral cell lines, and the ability of these compounds to stimulate mouse peritoneal macrophages in culture to become tumoricidal (indirect toxicity) was also studied. Direct cytotoxic activity was very low for all derivatives. However, almost all compounds showed a remarkable increase of indirect cytotoxicity. In particular, compound 3i, which has an F atom in the 7 position of the flavone ring, was able to increase significantly the macrophage's lytic properties, and has been selected for further investigations.</p>","PeriodicalId":7927,"journal":{"name":"Anti-cancer drug design","volume":"13 8","pages":"881-92"},"PeriodicalIF":0.0000,"publicationDate":"1998-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anti-cancer drug design","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

Abstract

Some flavone-2'-carboxylic acid analogues are described. Direct in vitro toxicity of the synthesized compounds was evaluated towards four tumoral cell lines, and the ability of these compounds to stimulate mouse peritoneal macrophages in culture to become tumoricidal (indirect toxicity) was also studied. Direct cytotoxic activity was very low for all derivatives. However, almost all compounds showed a remarkable increase of indirect cytotoxicity. In particular, compound 3i, which has an F atom in the 7 position of the flavone ring, was able to increase significantly the macrophage's lytic properties, and has been selected for further investigations.

分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
黄酮-2′-羧酸类似物作为潜在抗肿瘤药物的合成。
介绍了一些黄酮-2′-羧酸类似物。研究了合成的化合物对四种肿瘤细胞系的直接体外毒性,并研究了这些化合物刺激培养的小鼠腹腔巨噬细胞成为杀瘤细胞的能力(间接毒性)。所有衍生物的直接细胞毒活性都很低。然而,几乎所有化合物都表现出显著的间接细胞毒性。特别是化合物3i,在黄酮环的7位有一个F原子,能够显著增加巨噬细胞的裂解性能,并被选中进行进一步的研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 去求助
来源期刊
自引率
0.00%
发文量
0
期刊最新文献
Linker length in podophyllotoxin-acridine conjugates determines potency in vivo and in vitro as well as specificity against MDR cell lines. Topoisomerase I/II selectivity among derivatives of N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA). Synthesis and anticancer activity of nordihydroguaiaretic acid (NDGA) and analogues. Cyclohexylamino-demethoxy-hypocrellin B and photodynamic therapy decreases human cancer in vitro. Photokilling of cultured tumour cells by the porphyrin derivative CF3.
×
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
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 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 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1