A new series of N-aryl-N'-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)ureas bearing an alkoxycarbonylamino group at the 6-position were synthesized and examined as putative anticancer agents targeting sirtuins in glioma cells. Based on computational docking combined to in vitro sirtuin 1/2 inhibition assays, we selected compound 18 [R/S-N-3-cyano...
Cardiac glycosides (CGs) are approved for the treatment of cardiovascular alterations and their known cellular target is the alpha subunit of the sodium (Na+)/potassium (K+)-ATPase (NKA). Pharmacologically, they represent a well-known generation of drugs for treating cardiovascular problems, thus allowing the investigation of potential dose-depende...
Seven new (1–3, 5 and 8–10) and three previously reported (4, 6 and 7) 4α-methylated steroids were isolated from the organic extract of the gorgonian Litophyton mollis. The structures and the relative configurations of the isolated natural products were determined on the basis of extensive analyses of their NMR and MS data. Metabolites 1 and 5...
The remarkable complexity of cancer involving multiple mechanisms of action and specific organs led researchers Hanahan and Weinberg to distinguish biological capabilities acquired by cancer cells during the multistep development of human tumors to simplify its understanding. These characteristic hallmarks include the abilities to sustain prolifera...
The Eighth Central European Conference “Chemistry towards Biology” was held in Brno, Czech Republic, on 28 August–1 September 2016 to bring together experts in biology, chemistry and design of bioactive compounds; promote the exchange of scientific results, methods and ideas; and encourage cooperation between researchers from all over the wor...
In vitro and in vivo studies reported the anti-cancer potential of organosulfur compounds (OSCs) as they trigger biological effects leading to cell cycle arrest with accumulation of cells in G2/M, alteration of the microtubular network, modulation of Bcl-2 family protein expression patterns and changes of the redox status. Despite these well-descri...
We characterized the brominated alkaloid Isofistularin-3 (Iso-3), from the marine sponge Aplysina aerophoba, as a new DNA methyltransferase (DNMT)1 inhibitor. Docking analysis confirmed our in vitro DNMT inhibition data and revealed binding of Iso-3 within the DNA binding site of DNMT1. Subsequent increased expression of tumor suppressor gene aryl ...
Cancer and aging are two similar processes representing the final outcome of time-dependent accumulation of various irreversible dysfunctions, mainly caused by stress-induced DNA and cellular damages. Apoptosis and senescence are two types of cellular response to damage that are altered in both cancer and aging, albeit through different mechanisms....
Aim: To investigate the cytotoxic effect of methanol extract of Ptreocarpus erinaceus stem barks against cancer lines (Leukemia cell K562 and lung small cells A549) and its inhibition effects against NF-kB activation and lipoxygenase enzyme. Moreover, phenolic compounds, tannins and flavonoids amounts have been determined. Study Design: In vitro ev...