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Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies.
(2019-12-01)
A large library of fibrate-based N-acylsulphonamides was designed, synthesised, and fully characterised in
order to propose them as zinc binders for the inhibition of human carbonic anhydrase (hCA) enzymatic
activity. ...
Preparation of single chain nanoparticles via photoinduced radical coupling process
(2019-04-01)
This contribution introduces a straightforward method for preparing well-defined polymeric nanoparticles using radical coupling process of ketyl moieties resulted from triplet excitation of pendant benzophenone groups. In ...
Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme.
(2019-12-01)
Inhibition of the b-carbonic anhydrase (CA, EC 4.2.1.1) from pathogenic Candida glabrata (CgNce103) by
1H-indole-2,3-dione 3-[N-(4-sulfamoylphenyl)thiosemicarbazones] 4a–m was investigated. All the compounds were found ...
Noscapine, a Non-addictive Opioid and Microtubule-Inhibitor in Potential Treatment of Glioblastoma
(2019-08-01)
Noscapine is a phthalide isoquinoline alkaloid that easily traverses the blood brain barrier and has been used for years as an antitussive agent with high safety. Despite binding opioid receptors, noscapine lacks significant ...
Chemical Investigation and Bioactivity Screening of Salvia cassia Extracts
(2019-03-01)
In this study the antioxidant and anticholinesterase activities of the crude ethanol extract, as well as the dichloromethane and water extracts obtained from partitioning of the crude ethanol extract, of the plant Salvia ...
Indole-Based Hydrazones Containing A Sulfonamide Moiety as Selective Inhibitors of Tumor-Associated Human Carbonic Anhydrase Isoforms IX and XII
(2019-05-01)
Novel sulfonamidoindole-based hydrazones with a 2-(hydrazinocarbonyl)-3-phenyl-1Hindole-5-sulfonamide scaffold were synthesized and tested in enzyme inhibition assays against the
tumor-associated carbonic anhydrase isoforms, ...
Aromatase inhibition by 2-methyl indole hydrazone derivatives evaluated via molecular docking and in vitro activity studies.
(2019-05-01)
A causal association is reported between prolonged exposures to elevated levels of estrogen and breast cancer. Therefore inhibiting aromatase (CYP19A), which catalyses the conversion of androgens to estrogens, is an important ...