Preparations of cis- and trans-platinum(II) complexes of diethyl (pyridin-4-ylmethyl)phosphate (4-pmOpe) have been described. These complexes were identified and characterized by far-IR, 1H NMR, 13C NMR, 31P NMR and 195Pt NMR and microanalyses. The crystal and molecular structure of trans-platin...

We report the hitherto unreported pyrene footed calix[4]resorcinarene (P1) supramolecular assembly and its tetranuclear Ru(II) polypyridyl complexes, [{Ru(phen)2}4(L)](ClO4)8 (CP1), [{Ru(bpy)2}4(L)](ClO4)8 (CP2), and [{Ru(P2)2}4(L)](ClO4)8 (CP3) [where, L = 2,8,14,20-tetra(pyren-1-yl)-5,11,17,23...

The design, modeling, synthesis and biological activity evaluation of two hybrid agents formed by 7-oxyiminomethylcamptothecin derivatives and diaminedichloro-platinum (II) complex are reported. The compounds showed growth inhibitory activity against a panel of human tumor cell lines, including ...

The novel guanidine compounds trans-[Pt(NH2Me)2{NH=C(NHMe)NR}2](Cl)2 (R = NEt2 [7], NC5H10 [8]) (trans-7,8) were synthesized by the nucleophilic addition of methylamine to dialkylcyanamide ligands of the push–pull nitrile complexes trans-[PtCl2(RCN)2] (R = NEt2, NC5H10). In vitro cytotoxicity t...

The substitution kinetics of the complexes [Pt(II)(bis(2-pyridylmethyl)amine)H2O](ClO4)2, Ptdpa and [Pt(II)(bis(2-pyridylmethyl)sulfide)H2O](ClO4)2, Ptdps, with a series of azole nucleophiles: Imidazole (Im), 1-methylimidazole (MIm), 1,2-Dimethylimidazole (DIm), 1,2,4-triazole (Trz) and pyrazole...

A new synthesis of cis-dichlorobis(methylamine)platinum(II) is described. It appears that during the crystallization process at least two types of crystals are formed. Form A is monoclinic with space group P2 1/n and unit cell dimensions a = 6.272, b = 15.726, c = 7.419Å, β = 99.86°, V = 721Å ...

A novel platinum complex with 1,3-bis(2,6-diisopropylphenyl)-1,3-dihydro-2H-imidazol-2-ylidenyl ligand has been synthesized and characterized on the basis of elemental analysis, MS, 1H and 13C NMR spectroscopy, X-ray Absorption Spectroscopy and single crystal X-ray diffraction studies. The XRD d...

A palladium-catalyzed dehydrogenative acylation of indoles using easily accessible aldehydes as the acyl source is described. This reaction provides a new approach for the synthesis of 3-acylindoles.

Ethyl (R)-4-chloro-3-hydroxybutanoate ester [(R)-CHBE] is an important chiral intermediate for the synthesis of chiral drugs. In this study, a novel short-chain, NADH-dependent dehydrogenase (LCRIII) from Lactobacillus curieae S1L19 was discovered to exhibit high activity and enantioselectivity ...

A number of 7H,9H-quinazolino[3,2-b]benz[d,e]isoquinolin-7-one derivatives containing chlorine atoms, methoxy, nitro or amino groups at the 11 or 12 position of the molecule skeleton have been synthesised.The structure of the dyes obtained has been confirmed by elemental analysis, as well as by ...

In order to ascertain which residues in heparin may be responsible for its metal binding capacities we have investigated metal binding to some of its component monosaccharides by 1H and 13C NMR. The diamagnetic Zn ion and the paramagnetic Ni ion were used as probes. 4-Methylumbelliferyl-2-deoxy-...

Entomopathogenic fungi are important natural regulatory factors of insect populations and have potential as biological control agents of insect pests. The cosmopolitan soil fungus Conidiobolus coronatus (Entomopthorales) easily attacks Galleria mellonella (Lepidoptera) larvae. Prompt death of in...

Steroid sulfatase (STS) regulates the formation of active steroids from systemic precursors, such as estrone sulfate and dehydroepiandrosterone sulfate (DHEAS). In breast tissues, this pathway is a source for local production of estrogens, which support the growth of endocrine-dependent tumours....

Sulfated sialic acid (SiaS) is a unique sialic acid (Sia) derivative in which an additional anionic group is attached to a carboxylated monosaccharide. Very little is known about the occurrence and biologic function of SiaS, due to the limitations of analytical methods to detect it in minute amo...

Important reactions of drug metabolism, including UGT mediated glucuronidation and steroidsulfatase mediated hydrolysis of sulfates, take place in the endoplasmic reticulum (ER) of hepatocytes. Consequently, UGT generated glucuronides, like estradiol-17β-glucuronide, have to be translocated bac...

Efflux transport is a critical determinant to the pharmacokinetics of sulfate conjugates. Here we aimed to establish SULT1A3 stably transfected HEK293 cells, and to determine the contributions of BCRP and MRP transporters to excretion of chrysin and apigenin sulfates. The cDNA of SULT1A3 was sta...

LC–MS/MS has been proposed in various areas such as Therapeutic Drug Monitoring (TDM), Human Biomonitoring (HBM), disease diagnosis, clinical toxicology and doping control to identify and quantify chemical parents and their metabolites in biological matrices. To determine the total content of a...

The synthesis of hyaluronan dimers and tetramers equipped with a 4-methylumbelliferyl group at the reducing end to potentially allow monitoring of hyaluronidase activities is described. The 4-OH at the non-reducing glucuronate in the presented series is either removed or methylated to prohibit t...

Screening of large enzyme libraries such as those derived from metagenomic sources requires sensitive substrates. Fluorogenic glycosides typically offer the best sensitivity but typically must be used in a stopped format to generate good signal. Use of fluorescent phenols of pKa

The structure of oxalyl bromide (COBr)2 in the ground and four lowest excited electronic states was theoretically investigated using the CASPT2/cc-pVTZ-DK method. Structural information obtained allowed the reassignment of the A˜1Au←X˜1Ag and a˜3Au←X˜1Ag vibronic absorption spectra. Generaliza...