Myxochelin‐Inspired 5‐Lipoxygenase Inhibitors: Synthesis and Biological Evaluation
Sign Up to like & getrecommendations! Published in 2017 at "ChemMedChem"
DOI: 10.1002/cmdc.201600536
Abstract: A total of 48 analogues of the natural product myxochelin A were prepared and evaluated for their inhibitory effects on human 5‐lipoxygenase in both cell‐free and cell‐based assays. Structure–activity relationship analysis revealed that the secondary alcohol… read more here.
Keywords: inhibitors synthesis; myxochelin inspired; inspired lipoxygenase; myxochelin ... See more keywords
Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.07.069
Abstract: This paper describes the rational development of a series of novel spiroindoline derivatives endowed with selective inhibitory activity on the HDAC6 isoform. A convenient multicomponent one-pot protocol was applied for the assembly of the desired… read more here.
Keywords: inhibitors synthesis; hdac inhibitors; novel spiroindoline; spiroindoline hdac ... See more keywords
N-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1706503
Abstract: Abstract A urease inhibitor with good in vivo profile is considered as an alternative agent for treating infections caused by urease-producing bacteria such as Helicobacter pylori. Here, we report a series of N-monosubstituted thioureas, which… read more here.
Keywords: inhibitors synthesis; synthesis sar; sar biological; urease inhibitors ... See more keywords
Natural products as sources of acetylcholinesterase inhibitors: Synthesis, biological activities, and molecular docking studies of osthole-based ester derivatives
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Plant Science"
DOI: 10.3389/fpls.2022.1054650
Abstract: Osthole is a natural coumarin compound which isolated from Cnidium monnieri (L.) Cusson, has extensive pharmacological activities and could be used as a leading compound for drug research and development. In a continuous effort to… read more here.
Keywords: molecular docking; acetylcholinesterase inhibitors; natural products; inhibitors synthesis ... See more keywords
Arylaminopropanone Derivatives as Potential Cholinesterase Inhibitors: Synthesis, Docking Study and Biological Evaluation
Sign Up to like & getrecommendations! Published in 2020 at "Molecules"
DOI: 10.3390/molecules25071751
Abstract: Neurodegenerative diseases in which the decrease of the acetylcholine is observed are growing worldwide. In the present study, a series of new arylaminopropanone derivatives with N-phenylcarbamate moiety (1–16) were prepared as potential acetylcholinesterase and butyrylcholinesterase… read more here.
Keywords: inhibitors synthesis; potential cholinesterase; study; arylaminopropanone derivatives ... See more keywords
Pyrazole derivatives as potent EGFR inhibitors: synthesis, biological evaluation and in silico and biodistribution study.
Sign Up to like & getrecommendations! Published in 2022 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2022-0242
Abstract: Aim: Synthesis of pyrazole derivatives as EGFR inhibitors. Materials & methods: Cytotoxicity and EGFR inhibitory effect were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and EGFR kits, respectively. The biodistribution of radioiodinated compound nanoparticles in tumor-bearing mice was… read more here.
Keywords: derivatives potent; biodistribution; egfr inhibitors; inhibitors synthesis ... See more keywords