This article describes the synthesis and characterization of new 3'-triazolyl-5'-aryl-chalcogenothimidyne derivatives. Sulfur, selenium, and tellurium nucleosides were prepared from commercial zidovudine, using a linear synthetic strategy affording these compounds in good yields. The respective molecules were evaluated for cytotoxicity in bladder carcinoma 5637 cells and as an antioxidant agent, showing a linear dependence on the chalcogenium atom for both biological approaches. Tellurium was the most active element, followed by selenium and sulfur.
A straightforward and high-yielding methodology for the synthesis of a high structural diversity of 1,2,4-oxadiazoles from different chiral N-protected α-amino acids and amidoximes under microwave (MW) irradiation is described herein. This greener approach gives the desired products using acetone/water as solvent in very short reaction times.
This article discloses the synthesis and biological in vitro activity of a novel class of compounds derived from 5′‐arylchalcogenyl‐3‐(phenylselanyl‐triazoyl)‐thymidine as antitumor agents in the 5637 bladder carcinoma. The synthesis of the new molecules obtained good yields and proved to be efficient. The antitumor biological property, which was presented by a series of these unpublished compounds, demonstrates the importance of the presence of the nucleoside portion and the chalcogenium atom in the molecule.
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