60049-53-8Relevant academic research and scientific papers
Discovery of Novel Naphthylphenylketone and Naphthylphenylamine Derivatives as Cell Division Cycle 25B (CDC25B) Phosphatase Inhibitors: Design, Synthesis, Inhibition Mechanism, and in Vitro Efficacy against Melanoma Cell Lines
Cerchia, Carmen,Nasso, Rosarita,Mori, Matteo,Villa, Stefania,Gelain, Arianna,Capasso, Alessandra,Aliotta, Federica,Simonetti, Martina,Rullo, Rosario,Masullo, Mariorosario,De Vendittis, Emmanuele,Ruocco, Maria Rosaria,Lavecchia, Antonio
, p. 7089 - 7110 (2019/08/20)
CDC25 phosphatases play a critical role in the regulation of the cell cycle and thus represent attractive cancer therapeutic targets. We previously discovered the 4-(2-carboxybenzoyl)phthalic acid (NSC28620) as a new CDC25 inhibitor endowed with promising anticancer activity in breast, prostate, and leukemia cells. Herein, we report a structure-based optimization of NSC28620, leading to the identification of a series of novel naphthylphenylketone and naphthylphenylamine derivatives as CDC25B inhibitors. Compounds 7j, 7i, 6e, 7f, and 3 showed higher inhibitory activity than the initial lead, with Ki values in the low micromolar range. Kinetic analysis, intrinsic fluorescence studies, and induced fit docking simulations provided a mechanistic understanding of the activity of these derivatives. All compounds were tested in the highly aggressive human melanoma cell lines A2058 and A375. Compound 4a potently inhibited cell proliferation and colony formation, causing an increase of the G2/M phase and a reduction of the G0/G1 phase of the cell cycle in both cell lines.
Synthesis and studies on biological activities of some substituted 2-benzopyran-1H-one, 1H-2-oxo-benzopyran-3-carboxylic acids and 2-benzofuran- 1(H)-one
Purohit
, p. 222 - 227 (2007/10/03)
Prompted by the varied biological and herbicidal properties, the title compounds have been conveniently prepared by refluxing o-acyl/aroylbenzoic acids 1a-c / 4a-f with substituted / unsubstituted phenacyl bromides 2a-e or diethyl bromomalonate 7 in ethyl methyl ketone in the presence of potassium carbonate. All the compounds have been screened for different biological activities. The compounds 3b-e,i, 5b,d,f, and 8a,b show significant blood pressure effect on rats in vivo whereas spasmodic contraction is shown by 3c,e,i, and 5f in rat illium in vitro. Blood anticoagulant activity, bleeding time/clotting time has also been recorded for a few compounds 3a,c,e,i. A few isocoumarins 3d,e,h,i,g have been examined against different kinds of microbes. Phthalides 5a-e show remarkable results in growth and germination of seeds pigeon pea (Tuvar Var ICP) and tritieum estium (Wheat) in the recorded period.
