Arjun Basnet

2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure–activity relationship, and docking study

For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.

Identification of 1-furan-2-yl-3-pyridin-2-yl-propenone, an anti-inflammatory agent, and its metabolites in rat liver subcellular fractions

Abstract1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) has been characterized to have an anti-inflammatory activity through the inhibition of the production of nitric oxide and tumor necrosis factor-α. In the present studies, the phase 1 metabolism of FPP-3 was investigated in rat liver microsomes and cytosols. When FPP-3 was incubated with rat liver microsomes and cytosols in the presence of NADPH, 2 major peaks were detected on a liquid chromatography/electrospray ionization-mass spectrometry. Two metabolites (i.e., M1 and M2) were characterized as reduced forms on propenone: M1 (1-furan-2-yl-3-pyridin-2-yl-propan-1-one) was the initial metabolite and M2 (1-furan-2-yl-3-pyridin-2-yl-propan-1-ol) was a secondary alcohol believed to be formed from M1.

Design, synthesis and anticonvulsive activities of potential prodrugs linked by two-carbon chain

For the development of new anticonvulsive agents, GABAmimetics such as nipecotic acid, isonipecotic acid, γ-aminobutyric acid (GABA), γ-vinyl GABA (vigabatrin) and valproic acid were covalently coupled through an ester bond by a two-carbon linker chain as potential prodrugs and evaluated for their anticonvulsive activities.