1,2,3-Triazole tethered 2-mercaptobenzimidazole derivatives: design, synthesis and molecular assessment toward C6 glioma cell line.

Glioblastoma multiforme (GBM) is an aggressive cancer with very limited clinical therapies. Herein, we have designed novel mercaptobenzimidazole derivatives () as multitarget antineoplastic drugs and assessed their antiproliferative profiles on an experimental model for GBM, the C6 glioma line. The target compounds were synthesized in few steps with reasonable yields (33-90%).

Beyond the "Lock and Key" Paradigm: Targeting Lipid Rafts to Induce the Selective Apoptosis of Cancer Cells.

For more than 40 years, the fluid mosaic model of cellular membranes has supported our vision of an inert lipid bilayer containing membrane protein receptors that are randomly hit by extracellular molecules to trigger intracellular signaling events. However, the notion that compartmentalized cholesterol- and sphingomyelin-rich membrane microdomains (known as lipid rafts) spatially arrange receptors and effectors to promote kinetically favorable interactions necessary for the signal transduction sounds much more realistic. Despite their assumed importance for the dynamics of ligand-receptor interactions, lipid rafts and biomembranes as a whole remain less explored than the other classes of biomolecules because of the higher variability and complexity of their membrane phases, which rarely provide the detailed atomic-level structural data in X-ray crystallography assays necessary for molecular modeling studies.

New insights into the chemistry and antioxidant activity of coumarins.

Coumarins are considered to be privileged structures due to their broad range of biological properties, including anticoagulant, anti-neurodegenerative, antioxidant, anticancer and antimicrobial activities. These interesting properties of coumarins can be ascribed to the chemical attributes of the 2H-chromen-2-one core; its aromatic ring can establish a series of hydrophobic, π-π, CH-π and cation-π interactions, and the two oxygen atoms in the lactone ring may hydrogen-bond to a series of amino acid residues in different classes of enzymes and receptors. Additionally, the double bond in the lactone helps to make the entire system planar, allows charge delocalization between the carbonyl group of the lactone and the aromatic ring and confers the characteristic fluorescence of this class of compounds, which can be explained by their preventing the trans-cis transformation of the double bond under ultraviolet (UV) irradiation.