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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
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
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume84Issue:9Pages:739-745
AbstractSeries 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.
KeywordBreast Cancer Cell Line Diethyl 2 Anticancer Activity 5-diaminothiophene-3 Antimicrobial Activity 4-dicarboxylate Ptp-1b Inhibitor
Funding OrganizationFunds 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
Indexed BySCI
Funding OrganizationFunds 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
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Cited Times:8[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/3739
Collection省部共建新疆特有药用资源利用重点实验室
Corresponding AuthorAisa, HA
AffiliationChinese 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
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.
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