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Stearoylethanolamide exerts anorexic effects in mice via downregulation of liver stearoyl‐coenzyme A desaturase‐1 mRNA expression
TLDR
The novel observation provided here that SEA reduces food intake in mice in a structurally selective manner, in turn, correlated with downregulation of liver SCD‐1 mRNA expression, has the potential of providing new insights on a class of lipid mediators with suitable properties for the pharmacological treatment of over‐eating dysfunctions.
Coumarin as attractive casein kinase 2 (CK2) inhibitor scaffold: an integrate approach to elucidate the putative binding motif and explain structure-activity relationships.
TLDR
It is discovered that coumarin moiety can be considered an attractive CK2 inhibitor scaffold and the most promising inhibitor, 3,8-dibromo-7-hydroxy-4-methylchromen-2-one (DBC), has been also crystallized in complex with CK2, and the experimental binding mode has been used to derive a linear interaction energy (LIE) model.
Quinazoline derivatives as potential anticancer agents: a patent review (2007 – 2010)
TLDR
A comprehensive review of the quinazolines patented in 2007 – 2010 as potential anticancer agents and the number of different targets of the patents considered in this review is demonstrated.
Exploring epidermal growth factor receptor (EGFR) inhibitor features: the role of fused dioxygenated rings on the quinazoline scaffold.
A number of dioxolane, dioxane, and dioxepine quinazoline derivatives have been synthetized and evaluated as EGFR inhibitors. Their cytotoxic activity has been tested against two cell lines
4-hydroxymethyl-1,6,8-trimethylfuro[2,3-h]quinolin-2(1H)-one induces mitochondrial dysfunction and apoptosis upon its intracellular oxidation.
TLDR
The results suggest that the direct action on mitochondria of HOFQ-oxidized products are responsible for their cytotoxicity, which might be exacerbated, but hardly determined, by photodynamic action and/or binding to DNA.
Psoralen derivatives as inhibitors of NF-κB/DNA interaction: synthesis, molecular modeling, 3D-QSAR, and biological evaluation.
TLDR
The identification of compound 29 as a potential candidate for the development of pharmaceutical strategies against the inflammatory phenotype of cystic fibrosis was identified through the prediction of the activity of 17 novel compounds.
BIOLOGICAL PROPERTIES OF SOME BENZOPSORALEN DERIVATIVES
TLDR
Results suggest that DNA topoisomerases are probably the target of these two benzopsoralens, which appear to be capable of inducing strong antiproliferative effects by two different mechanisms, by UV‐A irradiation and in the dark.
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