Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and antiinfluenza virus agents. Part
Bozorov, K (Bozorov, Khurshed); Zhao, JY (Zhao, Jiang Yu); Nie, LF (Nie, Li Fei); Ma, HR (Ma, Hai-Rong); Bobakulov, K (Bobakulov, Khayrulla); Hu, R (Hu, Rui); Rustamova, N (Rustamova, Nigora); Huang, GZ (Huang, Guozheng); Efferth, T (Efferth, Thomas); Aisa, HA (Aisa, Haji A.); Aisa, HA
2017
发表期刊RSC ADVANCES
卷号7期号:50页码:31417-31427
摘要

On the basis of high-throughput screening, fragment-based drug discovery, structure-activity relationships and building block analysis methods, herein we report the synthesis and biological evaluation of a novel series of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives. All of the prepared Schiff bases (with mono-, di-and poly-substituents at the aromatic portion), mono-and bis-amides of diethyl 2,5diaminothiophene- 3,4-dicarboxylate, were evaluated against various human cancer and non-cancerous (only for active compounds) cell lines, as well as influenza A (subtypes FM/1/47/H1N1, hanfang/359/95/ H3N2) and B (subtype jifang/13/97) viruses. The obtained results suggest that some selected compounds revealed promising antitumor and antiviral activities and may serve as lead compounds for further drug discovery and development.

DOI10.1039/c7ra04808d
收录类别SCI
WOS记录号WOS:000404076400032
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被引频次:1[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/365002/5098
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1.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, 40-1 South Beijing Rd, Urumqi 830011, Xinjiang, Peoples R China
2.Acad Sci Uzbek, Inst Chem Plant Subst, 77 Mirzo Ulugbek Str, Tashkent 100170, Uzbekistan
3.Univ Chinese Acad Sci, 19 A Yuquan Rd, Beijing 100049, Peoples R China
4.Johannes Gutenberg Univ Mainz, Inst Pharm & Biochem, Dept Pharmaceut Biol, D-555128 Mainz, Germany
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Bozorov, K ,Zhao, JY ,Nie, LF ,et al. Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and antiinfluenza virus agents. Part[J]. RSC ADVANCES,2017,7(50):31417-31427.
APA Bozorov, K .,Zhao, JY .,Nie, LF .,Ma, HR .,Bobakulov, K .,...&Aisa, HA.(2017).Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and antiinfluenza virus agents. Part.RSC ADVANCES,7(50),31417-31427.
MLA Bozorov, K ,et al."Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and antiinfluenza virus agents. Part".RSC ADVANCES 7.50(2017):31417-31427.
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