Synthesis and cytotoxicity of oxindoles dispiro derivatives with thiohydantoin and adamantane fragments

Abstract

An effective and highly regio- and diastereoselective one-pot synthesis of two types of dispiro heterocyclic systems (2-thioxodispiro[imidazolidine-4,3′-pyrrolidine-2′,3″-indoline]-2″,5-diones and 2-thioxodispiro[imidazolidine-4,3′-pyrrolidine-4′,3″-indoline]-2″,5-diones) comprising pyrrolidinyl-oxindole, thiohydantoin and adamantane moieties has been developed based on a 1,3-dipolar cycloaddition of azomethine ylides, generated from isatin and sarcosine or formaldehyde and sarcosine, to adamantane-containing electron-deficient alkenes. Several molecules have demonstrated a considerable cytotoxicity against A549, HEK293T, MCF7 and VA13 cancer cell lines. The possible mechanism of anticancer activity of the synthesized compounds based on literature data may be the inhibition of p53/MDM2 interaction; however, we did not observe significant p53 activation using a reporter construction in A549 cell line in the relevant concentration range.     

Synthesis and Molecular Structure of Binuclear ansa-Bis(amidinate) Ytterbium Complex [1,3-C6H4{NC(Ph)N(SiMe3)}2]3Yb2

Russian Journal of Coordination Chemistry - The exchange reaction of anhydrous YbCl3 with [1,3-C6H4{NC(Ph)N(SiMe3)}2Li2(THF)2]2 (I) (4 : 3 molar ratio, THF) gave ansa-bis(amidinate)...     

Investigation of 1-azabicycles

The composition of mixtures of epimeric 3-methylpyrrolizidines obtained by four methods was determined by gas-liquid chromatography (GLC). The data presented make it possible to select a method for the preparation of a mixture of isomers of 3-methylpyrrolizidine with predominance of trans- or cis-3,8-H-3-methylpyrrolizidine.See [1] for communication IX.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 329–331, March, 1973.     

Electromagnetic emission under uniaxial compression of ice: I. Identification of nonstationary processes of structural relaxation by electromagnetic signals

Discrete electromagnetic emission caused by a jump of plastic deformation and fracture of single-crystal and polycrystalline ice is revealed and investigated. An album of electromagnetic signals is compiled, which makes it possible, on the basis of the electromagnetic-signal shape, to identify and study the kinetics of mesoscopic events of structural relaxation that are related to the dynamics of dislocation pile-ups and cracks.     

Preparation of Platinum(II) Cyclooctadiene Complexes by Photoirradiation

Preparation of platinum cyclooctadiene complexes under photoirradiation was studied, and the reaction mechanism was suggested.__________Translated from Zhurnal Obshchei Khimii, Vol. 75, No. 3, 2005, pp. 353–356.Original Russian Text Copyright © 2005 by de Vekki, Uvarov, Skvortsov.     

Stability of the Face Layer of Sandwich Structures with a Local Interlaminar Damage

The effect of a local interlaminar damage on the stability of the face layer of composite sandwich beams is investigated. Mathematical models are proposed for estimating the critical compressive stresses for two typical types of damage. Experimental and numerical data are obtained for two types of materials (with glass-fiber-reinforced plastics as face layers and Rohacell WF51 and Divinycell H60 foams as the core). The analytical results agree well with the experimental data.