Identification of SVM-based classification model, synthesis and evaluation of prenylated flavonoids as vasorelaxant agents

Benzofuran–Morpholinomethyl–Pyrazoline Hybrids as a New Class of Vasorelaxant Agents: Synthesis and Quantitative Structure–Activity Relationship Study

“…This was in agreement with previous reports of vasorelaxant activity of the chalcone system. [49][50][51] Cyclization of compounds 3a-e to produce pyrazoline derivatives 4a-e resulted in slight decrease in activity as expressed with increase in IC 50 values (IC 50 0.5502-0.7625 mM).…”

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“…β-hematin formation inhibition activity (BHIA 50 ) of the pyrazolines were determined and correlated with antimalarial activity. A reasonably good correlation (r = 0.62) was observed between antimalarial activity (IC 50 ) and BHIA 50 . This suggested that antimalarial mode of action of this class of compounds appears to be similar to that of chloroquine and involves the inhibition of hemozoin formation.…”

“…The effect on the activity of the nuclear enzyme DNA topoisomerase II was also investigated. A noticeable cytotoxic effect was observed for all pyrroloquinoline-conjugated compounds particularly against human melanoma cell line JR8 (IC 50 1.2-3.3 μM); the unconjugated chalcones and butenone had a lower or no effect at the tested concentrations 31 . …”

“…Initially the acute toxicity of the compounds was assayed via the determination of their LD 50 . All the compounds were interestingly less toxic than the reference drug.…”

Synthesis and characterization of 5,7-dihydroxyflavanone derivatives as novel protein tyrosine phosphatase 1B inhibitors

“…1-(2,4,6-Trihydroxy-phenyl)-ethanone was treated with chloromethyl methyl ether and potassium carbonate in acetone at room temperature to produce 1-(2-hydroxy-4,6-bis-methoxymeth-oxy-phenyl)-ethanone 1. Intermediates 2a-n were prepared by Claisen-Schmidt condensation of 1 with appropriate aromatic aldehydes, followed by cyclization in refluxing ethanol in the presence of NaOAc, which yielded flavanones 3a-n. Demethoxymethylation of 3a-n was carried out in 5 M HCl in refluxing methanol to yield 4a-n 38,39 . The spectral data obtained from infrared spectroscopy, 1 H-NMR and mass spectrometry were consistent with the structures proposed.…”