Combinatorial Chemistry & High Throughput Screening - Volume 15, Issue 5, 2012

Protein methyltransferases (PMTs) orchestrate epigenetic modifications through post-translational methylation of various protein substrates including histones. Since dysregulation of this process is widely implicated in many cancers, it is of pertinent interest to screen inhibitors of PMTs, as they offer novel target-based opportunities to discover small molecules with potential chemotherapeutic use. We have thus developed a Read More

Dysfunction of P/Q-type calcium channels is thought to underlie a variety of neurological diseases. There is evidence that migraine, Alzheimer’s disease, and epilepsy involve a gain-of-function of the channel, leading to abnormal presynaptic vesicle release. P/Q-channel blockers may normalize current flow and consequently lead to an alleviation of disease symptoms. Although the medical need is high, there are no su Read More

Here we present a novel beaded chemically stable, highly permeable hydrophobic/hydrophilic balanced support for solid phase peptide synthesis. The resin (SPED) was prepared by free radical suspension polymerization using monomers styrene and 9-decen-1-ol with amphiphilic cross-linking agent polyethyleneglycol diacrylate (Mn≈ 258). Different cross-linking densities were prepared to check the extent of swelling in differen Read More

A simple one-pot method for the preparation of 7-amino-2,4-dioxo-5-aryl-1,2,3,4-tetrahydropyrido[2,3- d]pyrimidine-6-carbonitriles 4 from aromatic aldehydes, malononitrile and 4(6)-aminouracil in the presence of ZrO2 nanoparticles (ZrO2 NPs) as an efficient heterogeneous catalyst is described. The procedure has the advantages of high yields (86-97%), short reaction time (2h) and an environmentally friendly specificity....

A new multicomponent domino reaction for rapid and regioselective synthesis of highly functionalized benzo[h]naphtho[2,3-a]acridine-15,16(5H,14H)-diones has been established. The reaction can be conducted by using readily available and inexpensive substrates under microwave irradiation. The procedures are facile, avoiding timeconsuming and costly syntheses, tedious work-up and purifications of precursors as Read More

A novel protocol for rapid assemble of benzimidazole framework has been demonstrated. This method incorporated with light fluorous-tag provides a convenient method for diversification of benzimidazoles and for easy purification via fluorous solid-phase extraction (F-SPE) in a parallel manner. The key transformation of this study involves in situ reduction of aromatic nitro compound, amide formation, cyclization and aromatizati Read More

A number of polycyclic aromatic hydrocarbons (PAHs) have been shown to be toxicants, and induce carcinogenic and immunotoxic effects. As a model PAH agent, 7,12-dimethylbenz[a]anthracene (DMBA) was the strongest one tested in terms of its biological activities and biotransformation. A new and simple high-performance liquid chromatographic (HPLC) method with diode-array detection at 290 nm was developed and va Read More

Fifty-six ionic liquids were efficiently synthesized in parallel format under one-pot, solvent-free microwaveassisted synthesis. These compounds were evaluated as extracting agents of nitrogen-containing compounds from a real Diesel feed before being submitted to the hydrodesulfurization process to obtain ultralow sulfur Diesel. Our results showed that halogenated ionic liquids are an excellent alternative due to these ionic Read More

Three-component reaction of 1-(6-hydroxy-2-isopropenyl-1-benzofuran-yl)-1-ethanone, dialkyl acetylenedicarboxylates and isocyanides in water was described as efficient and green synthetic procedure for preparation of 9Hfuro[ 2,3-f]chromene-8,9-dicarboxylates in excellent yield. In these reactions, 1-(6-hydroxy-2-isopropenyl-1-benzofuranyl)- 1-ethanone was extracted from rhizomes of Petasites hybridus from northern Ira Read More