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首页> 外文期刊>RSC Advances >Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and anti-influenza virus agents. Part 2
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Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and anti-influenza virus agents. Part 2

机译：新型二氨基噻吩支架作为抗肿瘤和抗流感病毒药物的合成及体外生物学评价。第2部分

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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.
机译：在高通量筛选，基于片段的药物发现，结构-活性关系和构件分析方法的基础上，本文报道了一系列新颖的2,5-二氨基噻吩-3,4-二羧酸二乙酯系列化合物的合成和生物学评价。衍生品。对所有制备的席夫碱（在芳族部分具有单，双和多取代基），2,5-二氨基噻吩-3,4-二羧酸二乙酯的单酰胺和双酰胺进行了评估，以对抗各种人类癌症和非癌细胞（仅适用于活性化合物）细胞，以及甲型流感病毒（FM / 1/47 / H1N1亚型，汉方/ 359/95 / H3N2）和乙型流感病毒（吉方/ 13/97亚型）。获得的结果表明，一些选定的化合物显示出有希望的抗肿瘤和抗病毒活性，并且可以用作进一步药物发现和开发的先导化合物。

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