A novel 4-aminoindazole sulfonamide hit (13) was identified as a human CCR4 antagonists from testing a focussed library of compounds in the primary GTPγS assay. Replacing the indazole core with a pyrazolopyrimidine, and introduction of a methoxy group adjacent to the sulfonamide substituent, re...

Light-emitting fluorophores 1–10b based on aryl substituted benzo[1,2-b:4,3-b′]dithiophenes (BDT) and trithia[5]helicenes (T5H) have been synthesized using various combinations of Suzuki coupling, the Wittig, or McMurry reaction, and subsequent photocyclization of the dithienylethenes thus obt...

New silver complexes of general formula [Ag(O3SCF3)(PPh2{bzt})n] (n = 1–3, bzt = benzo[1,2-b;4,3-b′]dithiophene) have been synthesized and characterized. Spectroscopic studies shown neutral ligand fluxionallity, typical of silver(I) complexes. The solid state structure of the complexes was det...

Nitrosation of 7-oxabicyclo[2.2.1]hept-5-en-2-exo-ylmethyl amine (20) gave 7-oxabicyclo[2.2.1]hept-5-en-2-exo-methanol (22) whereas 7-oxabicyclo[2.2.1]hept-5-en-2-endo-ylmethylamine (21) afforded a 1:1 mixture of 7-oxabicyclo[3.2.1]oct-6-en-2-ols (23) and 8-oxabicyclo[3.2.1]oct-3-en-2-ols (24). ...

We isolated two new dihydrooxopyridine cross-links, oxodesmosine (OXD) and isooxodesmosine (IOXD) from the acid hydrolysates of the bovine aortic elastin. OXD and IOXD were identified to have N-substituted 1,2-dihydro-2-oxopyridine and N-substituted 1,4-dihydro-4-oxopyridine skeletons, respectiv...

The pharmacology of several commonly described 5-hydroxytryptamine (5-HT)2C receptor agonists was investigated in vivo and in vitro at rat 5-HT2A, 5-HT2B, and 5-HT2C receptors. The 5-HT2C receptor agonist, (S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine fumarate (Ro 60-0175), did not indu...

9-((6-Phenylpyridin-3-yl)methyl)-9H-carbazole and 9-((6-(4-fluorophenyl)pyridin-3-yl)methyl)-9H-carbazole were synthesized as ligands by attaching a carbazolyl group to the pyridine in 2-phenylpyridine and 2-(4-fluorophenyl)pyridine, respectively. Four different Ir(III) complexes were prepared u...

Inhibition of VEGFR-2 kinase has been highlighted as one of the well-defined strategies to suppress tumor growth via blockade of angiogenesis. Guided by the principles of bioisosteric replacement and pharmacophoric fragment migration, a series of novel quinoxalinone derivates were designed, synt...

Ethyl trimethylsilyldiazoacetate reacts smoothly with a variety of aldehydes at 0 °C in the presence of a catalytic amount of tetrabutylammonium fluoride to produce α-diazo-β-hydroxy esters in good to excellent yields. The resulting α-diazo-β-hydroxy esters can be stereoselectively transfor...

A novel series of amino acids conjugated quinazolinone-Schiff’s bases were synthesized and screened for their in vitro anticancer activity and validated by molecular docking and DNA binding studies. In the present investigations, compounds 32, 33, 34, 41, 42 and 43 showed most potent anticancer...

Novel six-coordinated octahedral Co(II) complex [C36H26Br2CoN7O5, 1] and Cr(III) complex [C36H26Br2CrN6O2, 2] were prepared by the chelation reaction of the ligand 4-methoxybenzaldehyde-6-bromo-2-naphthoyl acylhydrazone and 2-acetylpyridine with Co(NO3)2·6H2O or CrCl3·6H2O in ethanol, and it i...

In the course of our search for new anti-breast cancer agents, substituted phenanthrenes with basic amino side chains were synthesized and some of them showed remarkable antiproliferative activity against ER +ve MCF-7 cell line with IC50 in the range of 3.53–22.25 μM. One of the compounds 15ca...

A series of derivatives of 1-(4-octylphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one (3) and 1-(4-octylphenoxy)-3-(1H-tetrazol-1-yl)propan-2-one (4) was synthesized and tested for fatty acid amide hydrolase (FAAH) inhibitory potency and phase I metabolic stability. Introduction of certain substituents...

In guinea pig, primate and man, nitric oxide (NO)-induced regulation of myometrial smooth muscle contraction is distinct from other smooth muscles because cyclic guanosine 3′,5′-cyclic monophosphate (cGMP) accumulation is neither necessary nor sufficient to relax the tissue. To further our und...

Nitric oxide (NO), including NO free radicals (·NO) and peroxynitrite (OONO−), modulates the release of neurotransmitters from neuronal tissues. Although we reported that S-nitroso-cysteine stimulated noradrenaline release in brain slices, we now show that only S-nitroso-cysteine inhibits norad...

The intracellular homeostasis of zinc is postulated to be controlled by signaling through nitric oxide (NO). Administration of the NO donor S-nitrosocysteine (SNOC) caused a rapid drop in the fluorescence of the zinc-specific fluorescence of the zinc probe zinquin in C6 glioma cells. Tentatively...

The carcinogenic action of a set of N-nitroso compounds containing the 2-oxopropyl group was considered in relation to their metabolism and their activity as alkylating agents for DNA. In contrast with the great carcinogenic potency of methylnitrosourea and ethylnitrosourea, comparable with the ...

A comparative genetic study was undertaken on the testicular tissue of Drosophila with N,α-acetoxymethyl-N-methylnitrosamine (AcODMN) and its unsubstituted parent N,N-dimethylnitrosamine (DMN), to assess the role of intracellular metabolism on their mutagenicities. The relative genetic potencie...

At pH 7.35, N-(2-oxopropyl)-N-nitrosourea (OPNU) reacted with calf thymus DNA to yield O6-methylguanine, 7-methylguanine and 3-methyladenine. Kinetic measurements of the base catalyzed decomposition of OPNU and the extent of methylation of DNA by OPNU suggested that methylnitrosourea is not form...

A boron difluoride complex of 3-acetyl-5,7-di(pyrrolidin-1-yl)-4-hydroxycoumarin was synthesized and converted into polymethine dyes which included an anionic, symmetric cyanine and several merocyanine compounds. The spectral luminescent behaviour of the dyes was studied. As the electron-withdra...