Reaction of 2-bromo-1, 1, 2-trichloro-3, 3-dimethylcyclopropane with one mol.equiv. of methyl lithium at −90 to 0°C leads to 1,2-dichloro-3,3-dimethylcyclopropene. This is stable for several hours at 20°C in chloroform or benzene solution but in the presence of an electron-rich or electron-poo...

1,2-Dibromo-3,3-dimethylcyclopropene, generated by debromination of 1,1,2,2tetrabromo-3, 3-dimethylcyclopropane on reaction with methyllithium, ring-opens at 0–20°C to produce 1,2-dibromo-3-methylbut-2-en-1-ylidene. This is trapped by alkenes to give vinylcyclopropanes. In the case of electron...

1,2-Dehalogenation of tetrachlorocyclopropanes (5, X = Cl, OMe, NPri2, SAllyl) by methyl lithium leads to dichlorocyclopropenes (6, X = Cl, OMe, NPri2, SAllyl); the first two of these react with electron rich and electron poor alkenes at 20°C to give cyclopropanes which are apparently derived b...

A moderate elevation in reactive oxygen species (ROS) levels can generally be controlled in normal cells, but may lead to death of cancer cells as the ROS level in cancer cells is already elevated. Therefore, a ROS-generating compound can act as a selective chemotherapeutic agent for cancer cell...

Disopyramide as an antiarrhythmic agent has been used for treating ventricular tachycardia and metabolized into its major metabolite, mono-isopropyl-disopyramide, by CYP3A4. We developed a novel, selective, highly sensitive, accurate, rapid method using liquid chromatography-tandem mass spectrom...

We describe mild and selective iodination of various 8-substituted imidazo[1,2-c]pyrimidine-5(6H)-ones (ethenocytosines). Starting ethenocytosines were obtained by cyclization of 5-halogenocytosines with chloroacetaldehyde or by subsequent Suzuki–Miyaura cross-coupling between 8-iodoimidazo[1,2...

3-{1-[(4-Fluorophenyl)sulfonyl]-1H-pyrazol-3-yl}-2-methylimidazo[1,2-a]pyridine, 2a, was discovered in our chemical library as a novel p110α inhibitor with an IC50 of 0.67 μM, through screening in a scintillation proximity assay. Optimization of the substituents of 2a increased the p110α inhi...

Transformation of 3-(chloromethyl)azetidin-2-ones to azetidine-3-carboxylic acid esters is described. The readily available 3-(chloromethyl)azetidin-2-ones rearranged in good yields to azetidine-3-carboxylic acid esters on treatment with alkoxides. An alternative ring opening - ring closure proc...

A series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues have been discovered as novel NOP receptor agonists. Structure–activity relationships have been explored via N-3 substitution of the benzimidazol-2-one with a range of functionality. The N-methyl acetamide derivative (+)-7f was...

Glutamate dehydrogenase (GDH) catalyzes the oxidative deamination of L-glutamate and is important for several biological processes. For GDH inhibitor screening, we developed a novel mono-sulfonated tetrazolium salt (EZMTT), which can be synthesized using H2O2 oxidation and purified easily on sil...

Among five major anthocyanin compounds, delphinidin exhibited the most potent and selective cytocidal effect against HL-60, a trivalent arsenic (As(III))-resistant cell line. Co-treatment with delphinidin and As(III) resulted in the reduction of IC50 value for As(III) from 11.2 to 1.5 μM, which...

IntroductionThe aim of this study was to evaluate whether delphinidin is cytoprotective or cytotoxic in osteosarcoma cell lines, and to elucidate the underlying mechanisms.

We have designed novel tropinone-thiazole derivatives that showed high antiproliferative activity against a variety of cancer cell lines via caspase 3/7 activation mechanism. Among the derivatives, compounds 3b-3h were found to exhibit high activity against human leukemia (MV4-11), human lung ca...

The unsymmetrical CNN pincer ligand precursors 4 and 7b based on the structures of bicyclo[3.2.l]octane and bicyclo[3.3.l]nonane have been synthesized. The corresponding palladium pincer 5,6-membered complexes 5 and 9 were prepared by direct cyclopalladation of ligand precursors with Li2PdCl4 in...

We have synthesized and assessed the ability of symmetrical fluorobenzoins and fluorobenzils to inhibit mammalian carboxylesterases (CE). The majority of the latter were excellent inhibitors of CEs however unexpectedly, the fluorobenzoins were very good enzyme inhibitors. Positive correlations w...

Synthesis and anticonvulsant activity of new N-Mannich bases of 3-(2-fluorophenyl)- and 3-(2-bromophenyl)-pyrrolidine-2,5-diones have been described. Initial anticonvulsant screening was performed in mice after intraperitoneal administration in the maximal electroshock seizure test (MES) and sub...

A copper-catalyzed intramolecular C–N bond formation reaction of 3-amino-2-(2-bromophenyl)dihydroquinazolinones has been developed for the synthesis of indazolo[3,2-b]quinazolinones in moderate to good yields. The structure of the newly synthesized indazolo[3,2-b]quinazolinones was unambiguousl...

Herpes simplex virus type 1 (HSV-1) causes significant human diseases ranging from skin lesions to encephalitis, especially in neonates and immunocompromised hosts. The discovery of novel anti-HSV-1 drugs with low toxicity is required for public health. Arbidol hydrochloride (ARB) is an indole d...

Alginate nanofibers were prepared in the presence of poly(ethylene oxide) (PEO), a surfactant Pluronic F-127, and a model drug (ciprofloxacin hydrochloride, CpHCl), all mixed prior to electrospinning. It was demonstrated that addition of a carrier polymer (PEO) and a small amount of surfactant a...

In this study, membrane bioreactor (MBR) and microbial fuel cell (MFC) was coupled for wastewater treatment using a polyvinylidene fluoride (PVDF) coated carbon fiber cloth as cathode membrane. To generate more power and mitigate membrane fouling, granular activated carbon (GAC) was added as a d...