Synthesis and In vitro Study of Cytotoxic Activity of New Tetrazole-Containing 2,4-Diamino-1,3,5-triazine Derivatives

Russian Journal of General Chemistry - New tetrazole-containing derivatives of 2,4-diamino-1,3,5-triazine were synthesized. The cytotoxic activity of the obtained compounds against Huh-7 and HeLa...     

Natural-Like Spirocyclic Δα,β-Butenolides Obtained from Diazo Homophthalimides

α-Diazo homophotalimides were reacted with various propiolic acids on Rh₂(esp)₂ catalysis. The resulting propiolate esters were transformed into novel, heterocyclic Δ^α,β-spirobutenolides in good to excellent product yields. The approach represents a fundamentally novel entry into natural-like Δ^α,β-spirobutenolides present in many biologically active natural products as well as fully synthetic compounds endowed with diverse biological activities. The Δ^α,β-spirobutenolides thus obtained were shown to inhibit thioredoxin reductase, a selenocysteine enzyme target for cancer. Moreover, for the best compound in the series (TrxR IC₅₀ 1.49±0.08 μM), by using MALDI-TOF mass-spectrometry it was shown that it selectively binds selenocysteine in the presence of a 10-fold excess of cysteine. This validates the new compound as a promising lead for anticancer therapy development.     

A new tetrazole-containing 2-amino-4,6-di(aziridin-1-yl)-1,3,5-triazine derivative: synthesis,interaction with DNA,and antitumor activity

Russian Chemical Bulletin - ({5-[4,6-Di(aziridin-1-yl)-1,3,5-triazin-2-yl]amino}-2,2-dimethyl-1,3-dioxan-5-yl)-methyl 2-(5-phenyl-2H-tetrazol-2-yl)acetate was synthesized and characterized. The...     

Isothermal Calorimetric Titration of Human Serum Albumin with the Fullerene C60-L-Arginine Adduct

Russian Journal of General Chemistry - The interaction of the fullerene C60-L-arginine adduct with human serum albumin (HSA) has been studied by means of isothermal calorimetric titration at 298.15...