Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES known for its potent antitumor activity and plays significant role in senescent cell removal. In this study, we synthesized [11C-carbonyl]BPTES ([11C]BPTES) as positron emission tomography (PET) probe the first time assessed biodist...

In this paper we present the convenient syntheses of seven new phenyl hydrazin derivatives 8 (a-h). For this purpose, acenaphtho [1,2-e]-1,2,4-triazine-9(8H)-thione (3) was prepared, starting from acenaphthylene-1, 2-dione (1) and thiosemicabazide in good yield. The reaction of (3) with benzyl chloride resulted to synthesis of 9-(benzylthio)-acenaphtho[1,2-e]-1,2,4-triazines (5) that reacted wi...

The equilibrium constant of adduct formation between some triorganotin chloride of the type R3SnCl (R=C6H5, p-CH3C6H4, n-CH3)CH2)3, C6H5-CH2 and Lewis bases Cl¯, Br¯, and I¯, were measured in 50% v/v ethanol-water solvent spectrophotometrically. The average equilibrium co...

A novel acrylate monomer containing 4H-pyran-4-one and 1,2,3-triazole ring, {1-[4-(4-oxo-6-phenyl-4H-pyran-2-yl)benzyl]-1,2,3-triazol-4-yl}methyl acrylate was synthesized by the reaction of 2-{4-[(4-(hydroxymethyl)-1,2,3-triazol-1-yl)methyl]phenyl}-6-phenyl-4H-pyran-4-one with acryloyl chloride in the presence of triethylamine. The structure of the acrylate monomer was established on the basis ...

Newly synthesized tocainide analogs were tested for their state-dependent affinity and use-dependent behavior on sodium currents (INa) of adult skeletal muscle fibers by means of the Vaseline-gap voltage clamp method. The drugs had the pharmacophore amino group constrained in position alpha [N-(2,6-dimethylphenyl)pyrrolidine-2-carboxamide (To5)] or beta [N-(2,6-dimethylphenyl)pyrrolidine-3-carb...