Journal
RSC ADVANCES
Volume 7, Issue 50, Pages 31417-31427Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7ra04808d
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Funding
- National Natural Science Foundation of China (NSFC) [21550110495]
- Chinese Academy of Sciences President's International Fellowship Initiative [2016PT014]
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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 2,5diaminothiophene- 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.
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