Combinatorial Chemistry & High Throughput Screening - Volume 16, Issue 5, 2013

A new diagnostic and prognostic biomarker may be of value in the diagnostic panel, especially among cancer diseases. The aim of the study was to evaluate the osteopontin (OPN) level measurable in the tumour tissue in females with diagnosed breast cancer after mastectomy, and to confirm its suitability to serve as a prognostic biomarker of the cancer. The OPN tissue levels and the classical risk factors were determined in tw Read More

Potassium fluoride impregnated on natural zeolite as a new solid base system effectively catalyzes the coupling of thiophenols with electron-deficient fluoro-, chloro- and bromo-arenes in DMSO. This versatile and efficient solid base has been demonstrated to afford the corresponding desired products in good to excellent yields. This procedure provides a convenient, efficient and practical method for the preparation of Read More

The existence of preferred molecular scaffolds that possess inherent biological activity, called privileged structures, is now well recognized. Such privileged structures not only provide enhanced drug-like properties but also give new hits for developing leads. The synthesis of combinatorial libraries, especially with the insertion of privileged substructures into heterocyclic moieties containing nitrogen, provides for a greater pr Read More

In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, we have synthesized eighteen alkyl/alkenylacyloxy derivatives at the C-28 position adopting exo-configuration of toosendanin (3a-r) by the reaction of toosendanin with fatty acids in the presence of N,N'-diisopropylcarbodiimide and 4- dimethylaminopyridine. Their activity was preliminarily evaluated agai Read More

A library of new 2-alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines was efficiently synthesized from hydrazones and anhydrides under microwave irradiation and solvent-free conditions. Compared with the traditional procedure (100 equiv. of anhydride and 1.5-4 h of reaction time), the present methodology has the advantages of short reaction time (10-20 min), and avoiding excess of anhydride (only 1.5 equiv Read More

A theoretical study of substitution effect on an electrocyclization reaction was performed using DFT method at B3LYP level of theory with 6-311G** basis sets. Equilibrium molecular geometries and harmonic vibrational frequencies of the reactant, transition state (TS), and product were calculated. The considered rate constants and activation thermodynamic parameters were calculated. The results indicated the reactio Read More