Solvent extraction of zinc(II) from and into ammoniacal chloride media with trialkylmethylammonium chloride (Aliquat336) has been investigated in the presence and absence of trioctylphospine oxide (TOPO). The results indicate that zinc extraction with Aliquat336 is sensitive to pH and ammonia co...

The leaching kinetics of zinc silicate in ammonium chloride solution was investigated. The effects of stirring speed (150–400 r/min), leaching temperature (95–108 °C), particle size of zinc silicate (61–150 μm) and the concentration of ammonium chloride (3.5–5.5 mol/L) on leaching rate of ...

An efficient NNN pincer Ru(II)-catalyzed preparation of quinazolines via acceptorless dehydrogenative strategy has been developed. Under the optimized conditions, a broad range of substituted o-aminobenzyl alcohols and (hetero)aryl or alkyl nitriles were well tolerated to afford various 2-substi...

A series of novel 2,4-disubstituted quinazolines were synthesized and evaluated for their anti-tumor activity against five human cancer cells (MDA-MB-231, MCF-7, PC-3, HGC-27 and MGC-803) using MTT assay. Among them, compound 9n showed the most potent cytotoxicity against breast cancer cells. Co...

Toll-like receptors (TLRs) are promising targets for treatment of viral infections, autoimmune diseases, and cancers. Here, two new series of selective small-molecule TLR7 agonists with novel scaffolds and good selectivity over TLR8 are described, some with potencies in the low micromolar range....

Aurora kinases comprise a family of phosphoproteins performing multiple functions in mitosis and meiosis. Because Aurora kinase B (AURKB) expression is altered in aged oocytes and there is only limited information on its function in meiosis, it was decided to study the spatial distribution and c...

We review solar/geophysical data relating to the great magnetic storm of 14–15 May 1921, with emphasis on observations of the low-latitude visual aurora. From the reports we have gathered for this event, the lowest geomagnetic latitude of definite overhead aurora (coronal form) was 40° and the...

Two series of 20 novel 4-aminoquinazoline—urea derivatives have been designed and synthesized. The entire target compounds were investigated for their in vitro antiproliferative activity against six human cancer cell lines (K562, U937, A549, NCI-H661, HT29 and LoVo) using the MTT-based assay. M...

A practical preparation of nitroarylamines from protected arylamines was herein disclosed. In this system, sodium nitrite acted as a nitration reagent in the presence of sodium persulfate without any transition-metal catalysts. This efficient site-selective protocol took place at room temperatur...

The in situ generated highly electrophilic nitrile imines derived from trifluoroacetonitrile are efficiently trapped by monomeric mercaptoacetaldehyde at room temperature in THF solution. The initially formed 1:1 adducts undergo spontaneous cyclization leading to 6-membered 5,6-dihydro-1,3,4-thi...

The unique selective estrogen receptor modulator, Raloxifene (1), and antitubulin agent 2 were synthesized through the key intermediate, 4-methoxybenzyl 2-bromo-4-methoxyphenyl sulfoxide (6), respectively. It was found that compared with the o-sulfanyl aryl bromides, the sulfinyl group at ortho ...

In this work, a new class of highly potent antituberculosis agents, 1-substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their oxa and selanyl analogs, is described. The minimal inhibitory concentration (MIC) values reached 1 μM (0.36–0.44 μg/mL) against Mycobacterium tuberculosis ...

6-Chloro-3-((1-methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine (JHU85270), a novel high-affinity ligand for the α4β2 nicotine acetylcholine receptor (nAChR) (Ki=86, 115 pM; KiJHU85270/Kiepibatidine=1.7) with a log D7.4=1.6 was synthesized in 56% overall yield. [11C]JHU8527...

A novel series of 3,4-diaza-bicyclo[4.1.0]hept-4-en-2-ones were designed and synthesized as H3R analogs of irdabisant 6. Separation of the isomers, assignment of the stereochemistry by crystallography, and detailed profiling of diastereomers 25 and 26 led to the identification of (1R,6S)-5-{4-[3...

A series of 3-(N-alkyl-N-phenylamino)propan-2-ol derivatives were synthesized from epichlorohydrine in a multi-step strategy and were evaluated as Src kinase inhibitors. First, epoxy ring opening of epichlorohydrine was carried out in the presence of N-alkylanilines to yield 3-(N-alkyl-N-phenyla...

A series of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)acetamide (TTA) derivatives were synthesized and evaluated as potent inhibitors of HIV-1. Among the newly disclosed TTAs, compounds 7f, 7g and 7c were the most potent inhibitors of HIV-1 replication of the series (EC50 = 0.17 ± 0.02, ...

2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) valu...

Several 1-(phenoxycarbonyl)-1,2-dihydropyridines were prepared by the addition of alkylzinc iodides to 1-(phenoxycarbonyl)pyridinium salts.

Atom transfer radical polymerization conditions with copper(I) bromide/2,2′-bipyridine (Cu/2,2′-bpy) as the catalyst system were employed for the homopolymerization and random copolymerization of 1-phenoxycarbonyl ethyl methacrylate (PCMA) with methyl methacrylate (MMA). Temperature studies in...

The 1H and 13C NMR spectra of twelve phenyl acridine-9-carboxylates – alkyl-substituted in the phenyl fragment – and their 10-methyl-9-(phenoxycarbonyl)acridinium salts dissolved in CD3CN, CD3OD, CDCl3 and DMSO-d6 were recorded in order to examine the influence of the structure of these compou...