Bis(thiosemicarbazones) and their copper (Cu) complexes possess unique anti-neoplastic properties. However, their mechanism of action remains unclear. We examined the structure-activity relationships of twelve bis(thiosemicarbazones) to elucidate factors regarding their anti-cancer efficacy. Importantly, the alkyl substitutions at the diimine position of the ligand backbone resulted in two dist...

Simple isoquinoline alkaloids (heliamine, dehydroheliamine), a phthalide alkaloid noscapine, and an aporphine boldine are biosynthetically derived from amino acid tyrosine. These substrates simple synthetic (2-acetyl-7-amino-1,2,3,4-tetrahydroisoquinoline) contain nucleus. The biotransformation of these via reduction, oxidation, hydroxylation, N-oxidation reactions with different microorganism ...

A method is described that allows the in vivo differentiation of N-acetyl aspartate (NAA) from N-acetyl aspartyl glutamate (NAAG) by in vivo MR spectroscopy (MRS) at 3 Tesla (3T). The method, which is based on MEGA-point-resolved spectroscopy (PRESS) editing, selectively targets the aspartyl spin system of one species while deliberately removing the other species from the spectrum. This allows ...

The serine protease inhibitors diethyl p-nitrophenyl phosphate and phenylmethylsulfonyl fluoride (chemical modifiers of serine residue) and N-acetyl-l-tryptophan ethyl ester (competitive inhibitor of chymotryptic protease) inhibited 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (AGEPC; platelet-activating factor)-induced platelet aggregation and secretion. The inhibition was dependent on the p...

Five novel 3-alkyl-4-phenylacetylamino-4,5-dihydro-1H-1,2,4-triazol-5-ones (2) were synthesized by the reactions of 3-alkyl-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones (1) with phenylacetyl chloride and characterized by elemental analyses and IR, 1HNMR, 13C-NMR and UV spectral data. The newly synthesized compounds 2 were titrated potentiometrically with tetrabutylammonium hydroxide in four non-...

The formation of S-nitrosoglutathione (GSNO) from amyl nitrite and n-butyl nitrite was studied in rat liver microsomes, employing N-ethylmaleimide (MalNEt) as an activator and indomethacin as an inhibitor of microsomal glutathione S-transferase (GST). Rates were compared with GST activity measured with 1-chloro-2,4-dinitrobenzene (CDNB) as a substrate. MalNEt stimulated GST activity and the for...

Functionalization of a cobalt/dioxolene complex with branched, asymmetric alkyl chains promotes non-cooperative and cooperative valence tautomerisms synchronized with thermodynamically favoured crystal-to-melt and kinetically generated glass-to-melt phase transitions, respectively, depending on the degree of crystallinity.