Although platelets have been implicated in the pathogenesis of vascular diseases, little is known about factors that regulate interactions between platelets and the vessel wall under physiological conditions. The objectives of this study were to 1) define the contribution of nitric oxide (NO) to endotoxin (lipopolysaccharide, LPS)-induced platelet-endothelial cell (P/E) adhesion in murine intes...

A series of polycyclic fluorescent ligands were synthesised and evaluated in murine striatal synaptoneurosomes for N-methyl-D-aspartate receptor (NMDAR) mediated calcium flux inhibition and inhibition of calcium influx through voltage gated calcium channels (VGCC). Amantadine (a) and N-(1-adamantyl)-1,3-propanediamine (c) substituted with 1-cyanoisoindole (3), indazole (5), dinitrobenzene (7, 8...

Inhibition of the Chk1 kinase by small molecules binding to its active site is a strategy of great therapeutic interest for oncology. We report how computational modelling predicted the binding mode of ligands of special interest to the Chk1 ATP site, for representatives of an indazole series and debromohymenialdisine. These binding modes were subsequently confirmed by X-ray crystallography. Th...

The study of the role oncosuppressors in tumor transformations and death cells is an important aspect many areas biochemistry. One most well-known suppressors p53 protein. function protein to regulate expression genes whose products lead cell cycle arrest apoptosis. Many types cancer are associated with inactivation suppressor as a result mutation. p53Y220C oncogenic mutation it creates extende...

In the title compound, C(6)H(9)N(2) (+)·C(7)H(4)NO(4) (-), the nitro group of the 4-nitro-benzoate anion is twisted by 6.2 (2)° from the attached ring. In the crystal structure, the cations and anions are linked via strong N-H⋯O and weak C-H⋯O hydrogen bonds, forming a three-dimensional network.

Protein sulfenic acids are reactive, reversibly oxidized cysteinyl residues with roles in redox catalysis and regulation. Detection and quantification of these species in proteins is accomplished through chemical modification by reagents such as 7-chloro-4-nitrobenzo-2-oxa-1,3-diazole (NBD chloride), 2-nitro-5-thiobenzoate (TNB), dimedone, or derivatives of dimedone, followed by UV-visible spec...

In the title compound, C(18)H(13)NO(8)S(2), the nitro-phenyl ring forms dihedral angles of 46.67 (7) and 75.40 (6)° with the phenyl rings. The nitro group makes a dihedral angle of 26.13 (8)° with the attached ring. The crystal packing is stabilized by weak inter-molecular C-H⋯O hydrogen bonds.

The effect of nitric oxide synthase (NOS) inhibitors on the brain production of endogenous glutamate receptor antagonist, kynurenic acid, was estimated in vitro. Under standard incubation conditions N(G)-nitro-L-arginine, but not N(G)-nitro-L-arginine methyl ester, up to 5 mM, or 7-nitroindazole, up to 100 microM, inhibited de novo synthesis of kynurenic acid in cortical slices. However, during...

In the title compound, C(7)H(6)ClNO(2), the chloro, methyl and nitro substituents are situated next to each other in this order on the benzene ring, with the mean plane of the nitro group twisted away from the mean plane of the benzene ring by 38.81 (5)°.