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题名: 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
作者: 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.
通讯作者: Aisa, HA
关键词: Diethyl 2,5-diaminothiophene-3,4-dicarboxylate ; Breast cancer cell line ; Anticancer activity ; Antimicrobial activity ; PTP-1B inhibitor
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2014
DOI: 10.1016/j.ejmech.2014.07.065
卷: 84, 期:9, 页:739-745
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
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.
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内容类型: 期刊论文
URI标识: http://ir.xjipc.cas.cn/handle/365002/3739
Appears in Collections:新疆维吾尔自治区植物资源化学重点实验室 _期刊论文

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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(1000KB)期刊论文作者接受稿开放获取View 联系获取全文

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

Recommended Citation:
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.
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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
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