Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1
Bozorov, Khurshed; Ma, Hai-Rong; Zhao, Jiang-Yu; Zhao, Hai-Qing; Chen, Hua; Bobakulov, Khayrulla; Xin, Xue-Lei; Elmuradov, Burkhon; Shakhidoyatov, Khusnutdin; Aisa, Haji A.; Aisa, HA
2014
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号84期号:9页码:739-745
摘要Series of diethyl 2,5-diaminothiophene-3,4-dicarboxylate (DDTD) derivatives: azomethines of DDTD (2a- 1) have been synthesized and screened for their anticancer, antimicrobial and anti-diabetic activities. The novel synthesized compounds were characterized by H-1, C-13 NMR, MS and FT-IR analyses. All compounds were evaluated for their antiproliferative activity against three types of cancer cell line such as T47D and MCF-7 (human breast cancer), Hela (human cervical cancer) and Ishikawa (human endometrial cancer) lines. The results showed that most compounds exhibited significant antiproliferative activity against breast cancer cells. The majority of azomethines DDTD influenced strongly against breast cancer cells T47D and MCF-7, among them compounds 2b (2.3 mu M), 2c (12.1 mu M), 2e (13.2 mu M), 2i (14.9 mu M), 2j (16.0 mu M), 2k (7.1 mu M), 21(8.6 mu M) manifest potent anticancer activity against cancer cell T47D than Doxorubicin (DOX, 15.5 mu M). Compound 2j has shown potent activity on all three types of cancer cells concurrently and IC50 values were considerably low in comparison with positive control DOX. In addition, all compounds were tested for antimicrobial activity against Staphylococcus aureus ATCC 6538 (Gram positive bacteria), Escherichia coil ATCC 11229 (Gram negative bacteria) and Candida albicans ATCC 10231 (Fungi) strains and 2j which contains in the ring nitrofurfural fragment, showed the highest effect on the three species of microbial pathogens simultaneously. Some compounds induced enzymatic inhibition in a concentration-dependent manner on PTP-1B inhibitor.
关键词Breast Cancer Cell Line Diethyl 2 Anticancer Activity 5-diaminothiophene-3 Antimicrobial Activity 4-dicarboxylate Ptp-1b Inhibitor
资助者Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences ; Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences ; Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences ; Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences
DOI10.1016/j.ejmech.2014.07.065
收录类别SCI
资助者Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences ; Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences ; Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences ; Funds for International Cooperation and Exchange of the National Natural Science Foundation of ChinaCASCentral Asia Drug Research and Development Center of Chinese Academy of Sciences
引用统计
被引频次:6[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.xjipc.cas.cn/handle/365002/3739
专题省部共建新疆特有药用资源利用重点实验室
通讯作者Aisa, HA
作者单位Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, Urumqi 830011, Xinjiang, Peoples R China;Acad Sci Uzbek, Inst Chem Plant Subst, Tashkent 100170, Uzbekistan
推荐引用方式
GB/T 7714
Bozorov, Khurshed,Ma, Hai-Rong,Zhao, Jiang-Yu,et al. Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,84(9):739-745.
APA Bozorov, Khurshed.,Ma, Hai-Rong.,Zhao, Jiang-Yu.,Zhao, Hai-Qing.,Chen, Hua.,...&Aisa, HA.(2014).Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,84(9),739-745.
MLA Bozorov, Khurshed,et al."Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 84.9(2014):739-745.
条目包含的文件
文件名称/大小 文献类型 版本类型 开放类型 使用许可
Discovery of diethyl(1000KB)期刊论文作者接受稿开放获取CC BY-NC-SA浏览 请求全文
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Bozorov, Khurshed]的文章
[Ma, Hai-Rong]的文章
[Zhao, Jiang-Yu]的文章
百度学术
百度学术中相似的文章
[Bozorov, Khurshed]的文章
[Ma, Hai-Rong]的文章
[Zhao, Jiang-Yu]的文章
必应学术
必应学术中相似的文章
[Bozorov, Khurshed]的文章
[Ma, Hai-Rong]的文章
[Zhao, Jiang-Yu]的文章
相关权益政策
暂无数据
收藏/分享
文件名: Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity Synthesis and in vitro biological evaluation. Part 1.pdf
格式: Adobe PDF
此文件暂不支持浏览
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。