2-Aminothiophene scaffolds: Diverse biological and pharmacological attributes in medicinal chemistry
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Acknowledgments
This work was funded by grants from the National Natural Science Foundation of China (NSFC) (Grant No. 21550110495) and Chinese Academy of Sciences President’s International Fellowship Initiative (Grant No. 2016PT014). Abbreviations 2-ATs ― 2-aminothiophenes 3T3 ― mouse embryo fibroblast cell line A. fumigatus ― Aspergillus fumigatus A1AR ― A1 adenosine receptor A549 ― human lung cancer cell line ADME ― absorption, distribution, metabolism, and excretion AEs ― allosteric enhancers AKT ― protein kinase B AMPA ― α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid aPKC ― atypical protein kinase C AZT-TP ― azidothymidine triphosphate B. subtilis ― Bacillus subtilis Bcl-2 ― B-cell lymphoma 2 C. albicans ― Candida albicans CA-4 ― combretastatin A-4 cAMP ― cyclic adenosine monophosphate CB2 ― cannabinoid receptor type 2 CC50 ― half maximal cytotoxic concentration CCPA ― 2-chloro-N6-cyclopentyladenosine CD45 ― protein tyrosine phosphatase, receptor type, C CHO-K1 ― Chinese hamster ovary cells CYP51 ― cytochrome P450 lanosterol 14α-demethylase DCM – dichloromethane DIPEA ― N,N-diisopropylethylamine DMF – dimethylformamide DNA ― deoxyribonucleic acid DSF ― differential scanning fluorimetry E. coli ― Escherichia coli EC50 ― half maximal effective concentration ED50 ― effective dose, referring to the 50% population base ED90 ― effective dose, referring to the 90% population base ED99 ― effective dose, referring to the 99% population base EDCl ― 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide EDG ― electron-donating group EP2 ― prostaglandin E2 receptor 2 EP4 ― prostaglandin E2 receptor 4 ERK1/2 ― extracellular signal-regulated kinases 1 and 2 EWG ― electron-withdrawing group FFP ― fresh frozen plasma FluA ― influenza A virus G. candidum ― Geotrichum candidum GluR1 ― glutamate receptor 1 H1N1 ― the subtype of influenza A virus H3N2 ― the subtype of influenza A virus HCT-15 ― human colon cancer cell line HCTU ― 2-(6-chloro-1-H-benzotriazole-1-yl)-1,1,3,3-tetramethylaminium hexafluorophosphate HEK-293 ― human embryonic kidney 293 cells HeLa ― human epitheloid cervical carcinoma cells hERG ― human ether-a-go-go-related gene HIV ― human immunodeficiency virus HOBt ― 1-hydroxybenzotriazole HTS ― high-throughput screening IC50 ― half maximal inhibitory concentration IKK-β ― inhibitor of nuclear factor kappa-B kinase subunit beta IL-1 ― interleukin 1 beta JAK2 ― Janus kinase 2 JNK ― c-Jun N-terminal kinase Ki ― rate constant for the initial step in a radical reaction L. amazonensis ― Leishmania amazonensis L. donovani ― Leishmania donovani L-AlaDH ― alanine dehydrogenase LAR ― leukocyte common antigen – (LAR - related protein tyrosine phosphatases) LPS ― lipopolysaccharide LXR ― liver X receptor MCF-7 ― human breast cancer cell line (Michigan Cancer Foundation-7) Mcl-1 ― myeloid cell leukaemia 1 MDCK ― Madin-Darby canine kidney cells MDM2 ― mouse double minute 2 gene MDR-TB ― multi-drug-resistant tuberculosis MIC ― minimum inhibitory concentration MRSA ― methicillin-resistant Staphylococcus aureus MTB ― Mycobacterium tuberculosis mtFabH ― Mycobacterium tuberculosis beta-ketoacyl acyl carrier protein synthase III MurF ― muramyl ligase (UDP-N-acetylmuramoyl-tripeptide—D-alanyl-D-alanine ligase) NCI-60 ― National Cancer Institute 60 human tumour cell line NFB ― nuclear factor kappa-light-chain-enhancer of activated B cells NIH ― National Institutes of Health NMDA ― N-methyl-D-aspartate NMM ― 4-methylmorpholine NVP – nevirapine P. berghei ― Plasmodium berghei P. falciparum ― Plasmodium falciparum PANC-1 ― human pancreatic adenocarcinoma PA-PB1 ― polymerase acidic protein-basic protein 1 PBMC ― peripheral blood mononuclear cell PC-3 ― human prostate cancer cell line PDE4 ― phosphodiesterase type 4 PI3K ― phosphoinositide 3-kinase PPAR-γ ― peroxisome proliferator-activated receptor γ PS ― pantothenate synthetase PTP1B ― protein tyrosine phosphatase 1B PTPa ― protein phosphatase 2 phosphatase activator Py – pyridine RAW 264.7 ― mouse leukaemic monocyte macrophage cell line RNA ― ribonucleic acid RNAP ― ribonucleic acid polymerase R-PIA ― ribose-5-phosphate isomerase A RT ― reverse transcriptase RXRα ― retinoid X receptor α S. aureus ― Staphylococcus aureus S. cerevisiae ― Saccharomyces cerevisiae S. pneumoniae ― Streptococcus pneumoniae S. racemosum ― Syncephalastrum racemosum SAR ― structure-activity relationship SARMs ― selective androgen receptor modulators Sf9 ― Spodoptera frugiperda T. brucei brucei ― Trypanosoma brucei brucei T. cruzi ― Trypanosoma cruzi T1/2 ― terminal half-life T47D ― human breast cancer cell line TBAB ― tetra-n-butylammonium bromide TC PTP ― T-cell protein tyrosine phosphatase TEA – trimethylamine TFA ― trifluoroacetic acid THF – tetrahydrofuran TNF ― tumour necrosis factor TNF- ― tumour necrosis factor alpha TP53 ― tumour suppressor p53 VEGF ― vascular endothelial growth factor XDR-TB ― extensively drug-resistant tuberculosis β2-AR ― beta-2 adrenergic receptor Download 199.36 Kb. 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