Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113385
Abstract: An expanded series of alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates (HOPs) 3 was obtained via Cu(OAc)2-catalyzed azo coupling. All were nanomolar inhibitors of carboxylesterase (CES), while moderate or weak inhibitors of acetylcholinesterase and butyrylcholinesterase. Steady-state kinetics studies showed that… read more here.
Keywords: novel potent; carboxylesterase inhibitors; bifunctional carboxylesterase; inhibitors based ... See more keywords
Highly Selective and Potent Ectonucleotide Pyrophosphatase-1 (NPP1) Inhibitors Based on Uridine 5'-Pα,α-Dithiophosphate Analogues.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01906
Abstract: Ectonucleotide pyrophosphatase/phosphodiesterase-1 (NPP1) hydrolyzes phosphodiester bonds of nucleotides such as ATP, resulting mainly in the formation of AMP and pyrophosphate. NPP1 activity plays a deleterious function in calcified aortic valve disease and calcium pyrophosphate deposition… read more here.
Keywords: ectonucleotide pyrophosphatase; npp1; inhibitors based; uridine dithiophosphate ... See more keywords
Potent Metabolic Sialylation Inhibitors Based on C-5-Modified Fluorinated Sialic Acids
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.8b01757
Abstract: Sialic acid sugars on mammalian cells regulate numerous biological processes, while aberrant expression of sialic acid is associated with diseases such as cancer and pathogenic infection. Inhibition of the sialic acid biosynthesis may therefore hold… read more here.
Keywords: sialylation inhibitors; potent metabolic; inhibitors based; metabolic sialylation ... See more keywords
Recent studies on protein kinase signaling inhibitors based on thiazoles: review to date
Sign Up to like & getrecommendations! Published in 2024 at "RSC Advances"
DOI: 10.1039/d4ra05601a
Abstract: Due to the important role of protein kinases in protein phosphorylation within vital cellular processes, their abnormal function, especially in cancer situations, has underscored their importance in therapy. Thiazole structures are versatile frameworks present in… read more here.
Keywords: protein kinase; studies protein; kinase signaling; inhibitors based ... See more keywords
New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2020.1858820
Abstract: Abstract In the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity… read more here.
Keywords: steroid sulphatase; triazol naphthalen; inhibitors based; naphthalen sulphamate ... See more keywords
Structural Insight of New Butyrylcholinesterase Inhibitors Based on Benzylbenzofuran Scaffold
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15030304
Abstract: In the present work, we use a merger of computational and biochemical techniques as a rational guideline for structural modification of benzofuran derivatives to find pertinent structural features for the butyrylcholinesterase inhibitory activity and selectivity.… read more here.
Keywords: inhibitors based; structural insight; butyrylcholinesterase inhibitors; new butyrylcholinesterase ... See more keywords