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RESEARCH PRODUCT
Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and anti-influenza virus agents. Part 2
Haji Akber AisaLi Fei NieKhayrulla BobakulovKhayrulla BobakulovHai-rong MaKhurshed BozorovKhurshed BozorovThomas EfferthNigora RustamovaJiangyu ZhaoGuozheng HuangRui Husubject
010405 organic chemistryStereochemistryDrug discoveryChemistryGeneral Chemical EngineeringInfluenza aGeneral Chemistry010402 general chemistry01 natural sciencesIn vitroVirus0104 chemical sciencesCell cultureHuman cancerAnalysis methodBiological evaluationdescription
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 2,5-diaminothiophene-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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2017-01-01 | RSC Advances |