An unprecedented palladium-catalyzed chemoselective reduction and reductive amination of nitroarenes with water as a hydrogen source mediated by diboronic acid have been discovered. A series of aryl amines containing various reducible functional groups were obtained in good to excellent yields.

Curcumin (CUR) demonstrates a variety of biological activities; however, the poor oral bioavailability limits its clinical application. The objective of this study was to develop and evaluate characteristics and bioavailability of hollow microspheres loading curcumin (CUR-HPs). CUR-HPs were prep...

With water as the sole solvent, a green and efficient method has been developed for the synthesis of various α,α-dihaloketones via ultrasound assisted p-tolylthiourea catalyzed tandem reaction of alkynes with trihaloisocyanuric acids. This synthetic route could effectively avoid the use of tox...

In this paper, we report the synthesis and biological evaluation of a series of 1,5- and 1,4- substituted derivatives of 1H-imidazol-4-ylacetic acid, a series of 1,2-substituted 3-(1H-imidazol-2-yl)propanoic acid and an N-substituted (2E)-3-(1H-imidazol-2-yl)prop-2-enoic acid as new mGAT3 inhibi...

Inhibition of tumor angiogenesis through simultaneously disturbing vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) mediated signaling pathways is a well-established approach in intervention of tumor. A series of 6-methoxycarbonyl indolinones bearing a pyrrole ...

A new hydrazone ligand (2-(Methoxycarbonyl-hydrazono)-pentanedioic acid, H2L), derived from methyl carbazate and α-ketoglutaric acid, and its Ag(I) complex [Ag(HL)(H2L)] were synthesised and characterised by elemental, spectral and thermal analyses. The X-ray structures of the ligand and comple...

Cell extracts of Methanobacterium thermoautotrophicum (strain Marburg) were found to catalyze the reduction of the heterodisulfide of coenzyme M (CoM-S-H) and 7-mercaptoheptanoylthreonine phosphate (H-S-HTP) with H2. All the activity was associated with the soluble cell fraction (160 000 × g su...

The structure of component B of the methylcoenzyme M methylreductase system of Methanobacterium thermoautotrophicum was recently found to be 7-mercaptoheptanoylthreonine phosphate (HS-HTP). The work described here demonstrates that this compound is found in two forms: enzyme-free and enzymebound...

When 7-mercaptoheptanoylthreonine phosphate (HS-HTP) was used as the sole source of electrons for reductive demethylation of 2-(methylthio)-ethanesulfonic acid (CH3-S-CoM) by cell extracts of Methanobacterium thermoautotrophicum strain ΔH, the heterodisulfide of coenzyme M and HS-HTP (CoM-S-S-H...

The structure of component B of the methylcoenzyme M methylreductase system from Methanobacterium thermoautotrophicum was recently found to be 7-mercaptoheptanoylthreonine phosphate (HS-HTP). Three potential roles for this cofactor were considered. First, a methyl thioether derivative of the cof...

SummaryIn 40 western European patients with Stargardt disease (STGD), we found 19 novel mutations in the retina-specific ATP-binding cassette transporter (ABCR) gene, illustrating STGD's high allelic heterogeneity. One mutation, 2588G→C, identified in 15 (37.5%) patients, shows linkage dis...

A new series of 2-mercapto-quinazolin-4-one analogues was designed, synthesized and evaluated for their in vitro DHFR inhibition, antitumor and antimicrobial activity. Compound 17 proved to be the most active DHFR inhibitor with IC50 value of 0.01 μM, eight fold more active than methotrexate (M...

An efficient direct amination of quinazolin-4(3H)-ones has been developed. Treatment of quinazolin-4(3H)-ones with HCCP, DIPEA, and N-contained nucleophiles in acetonitrile could be able to form the corresponding 4-aminoquinazoline derivatives. Under the optimal reaction conditions, the aminatio...

A series of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives were designed, synthesized, and evaluated for their topoisomerase I and II inhibition and cytotoxic activity against several human cancer cell lines. Compounds 10–19 showed moderate topoisomerase I and II inhibitory activ...

The enzymatic kinetic resolution of the racemic alcohols 1-(3′-furyl)-3-buten-1-ol (±)-1 and 2-(2′-furyl)propan-1-ol (±)-2 was investigated by screening a range of lipases and esterases for enantioselective transacylation, as well as for enantioselective hydrolysis. For both alcohols, lipase...

N-(3-methoxypropyl)-N-(pyridin-2-ylmethyl)amine (abbreviated as mppma) and its complex [Mn(μ-Cl)2(mppma)]n have been synthesized. Single-crystal X-ray diffraction analysis has revealed that in the complex, mppma acts as a didentate ligand bound to the Mn(II) ion through two nitrogen atoms; [MnC...

Four titanium and zirconium complexes of (3-methoxypropyl)cyclopentadienyl, Cp′2MCl2 (M = Ti, Zr), Cp′CpTiCl2 and Cp′Cp″TiCl2 (Cp = C5H5, Cp′ = MeOCH2, CH2CH2C5H4, Cp″ = MeOCH2CH2C5H4), have been synthesized in good yields by reacting the potassium salt Cp′K with MCl4 (M = Ti, Zr), CpTiCl...

In order to identify a high-affinity, selective antagonist for the A2B subtype adenosine receptor, more than 40 1,8-disubstituted-3-(3-methoxypropyl) xanthines were prepared and evaluated for their binding affinity at recombinant human adenosine receptors, mainly of the A2A and A2B subtypes. Som...

In radiotherapy, dosimetry tools are needed to record and verify complex 3-D dose distributions. A novel composition of polymer gel dosimeter based on radiation-induced polymerization of N-(3-methoxypropyl) acrylamide (NMPA) is presented and studied as a 3-D dose verification quality assurance t...

Both free and bound fractions of polybrominated diphenyl ethers (PBDEs) and tetrabromobisphenol A (TBBPA) in sediment were examined. The free fraction was operationally defined as the fraction of each target compound extracted with a solvent mixture of hexane/acetone by Soxhlet extraction, while...