An improved one-pot van Leusen oxazole synthesis ..

Mechanism of Photochemical O-Atom Exchange in Nitrosamines with Molecular Oxygen
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A Practical Method for Oxazole Synthesis by …

Glycogen synthase kinase-3 (GSK-3) is associated with various key biological processes, including glucose regulation, apoptosis, protein synthesis, cell signaling, cellular transport, gene transcription, proliferation, and intracellular communication. Accordingly, GSK-3 has been implicated in a wide variety of diseases and specifically targeted for both therapeutic and imaging applications by a large number of academic laboratories and pharmaceutical companies. Here, we review the structure, function, expression levels, and ligand-binding properties of GSK-3 and its connection to various diseases. A selected list of highly potent GSK-3 inhibitors, with IC50 50

Synthesis of Polycyclic Heterocycles via Dess−Martin Periodinane-Mediated Cascade Cyclization: Generality, Scope, and Mechanism of the Reaction
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Chemistry of oxazoles - Chemical Reviews (ACS …

Gebhardt et al.[] showed application of emodin (82) and its ethylenediamine analog 83 as non-ATP competitive inhibitors of GSK-3 (Table ). Addition of the ethylenediamine group on the emodin nucleus increased potency of inhibition (IC50 0.56±0.02 µM, 83), reduced cytotoxicity and generated an insulin sensitizing effect mediated by increasing hepatocellular glycogen and fatty acid biosynthesis. Selectivity's of compounds 82 and 83 were evaluated against twelve protein kinases including eleven of human protein kinases. Compound 83 showed high selectivity towards GSK-3β but 82 failed to do so.

Van Leusen Reaction Involves the Conversion of Ketones into Nitrile. Learn about Van Leusen Reaction Mechanism, Oxazole and Imidazole Synthesis with …
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Oxazolines may also be synthesized by the reaction aromatic nitriles 23 with β-amino alcohols 24 using InCl3 as catalyst under reflux conditions 21. This catalyst can also be successfully applied to the chemo selective conversion of dicyanobenzenes to their corresponding mono- and bis-oxazolines. By using ultrasonic and microwave irradiation improve the yield and reduced the reaction time.

Synthesis of Oxazole Derivatives from Amides and Ketones.
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Classical oxazole synthetic methods in organic chemistry are

From Aldehydes 2-Oxazolines 19 also prepared by the reaction of aromatic aldehydes 18 with amino alcohol 17. This synthetic scheme is performed by many chemists using different catalyst. Shinde et al 17 were proposed a reaction scheme using NaBrO3 as catalyst.

Oxazole Synthesis from Isocyanides (PDF Download …

The latter compound is in general a by-product.

Robinson–Gabriel synthesis
Robinson–Gabriel synthesis
Reaction mechanism
The first part of this reaction is the cyclization of an 2-acylamidoketone that contains all three oxazole substituents.

Reactions of oxazoles (review) | SpringerLink

The product, which is the 2,5-disubstituted oxazole, precipitates as the hydrochloride and can be converted to the free base by the addition of water or by boiling with alcohol.

The cyanohydrins and aldehydes used for the synthesis are usually aromatic, however there have been instances where aliphatic compounds have been used.

2,5-dimethyl pyrazine, 123-32-0 - The Good Scents …

AB - Microtubule targeting agents are among the most widely used chemotherapeutics for both solid and hematological malignancies. This study characterizes the diaryl-oxazole based anticancer agent PC-046, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studies show that PC-046 is a synthetically-derived, small molecule microtubule destabilizing agent. Advantages over existing microtubule destabilizing agents include ease of synthesis, lack of MDR cross-resistance, good oral bioavailability and the lack of acute myelotoxicity.