The present work describes the preparation of a novel series of compounds based on the structure of goniothalamin (1), a natural styryl lactone with known cytotoxic and antiproliferative activities against a variety of cancer cell lines. A focused library of 17 goniothalamin analogues displaying...

Novel series of compounds consisting of 2-amidocyclohex-1-ene carboxylate and phenyl parts which are connected by enyne (compounds 2a–f), but-1-yne (compounds 4a–j), and phenylethylene (compounds 5a–f) linkers as HCA2 full agonists were designed and their functional activity using cAMP assay ...

The combination of an ‘ene’ reaction between a 2-(2-trialkylsilyloxyalkyl)prop-2-enyl(trimethyl)silane and an alk-1-yn-3-one mediated by zinc(II) iodide, and an intramolecular oxy-Michael reaction, provides an efficient synthesis of cis-2,6-disubstituted 4-methylenetetrahydropyrans of interest...

Concise and stereocontrolled syntheses of (+)-1-deoxynojirimycin and (2R,5R)-dihydroxymethyl-(3R,4R)-dihydroxypyrrolidine [(+)-DMDP] were achieved via a diastereomerically enriched oxazine intermediate. The key strategies include the use of 1,3-oxazine as a chiral building block and diastereosel...

The reaction of (E)-N,N,N-trimethyl-2-oxo-2-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)ethan-1-aminium-chloride (HLCl) with copper(II) perchlorate led to mononuclear [CuLCl]ClO4 complex (1). The same reaction with excess of sodium azide gives dinuclear azido double end-on bridged Cu(II) complex [...

The successful synthesis of new pyrimidine based organic ligands with terminal carboxylate and oxime functional groups, followed by their employment in metallogrid self-assembly has yielded three tetranuclear [Ni4(L1)4]∙2CH3CN∙4CH3OH·4H2O (1), [Cu4(HL1′)4]∙8CH3OH·28H2O (2) and [Ni4(H2L2)4](CF...

The aqua theophyllinate complexes of general formula [M(II)(Th)2(H2O)4] M(II) = Cd(II), Ni(II), Mn(II) and Cu(II), Th: theophyllinate, were prepared and characterized by the X-Ray diffraction analysis using the Fox program, infrared, UV–visible and TGA/DTA. These complexes were crystallized in ...

[email protected] was successfully fabricated and examined for Cu2+ adsorption from aqueous solutions. [email protected] was characterized by XRD, FT-IR, SEM, EDX and VSM. Furthermore, the effects of some factors such as pH, adsorbent type, Cu2+ concentration, adsorbent amount and time on adsorp...

Two methods for the chromatographic separation of technical 5-amino-4-chloro-2-phenyl-3(2H)-pyridazinone (PCA) were developed. These methods also permit the quantitative determination of its isomer (4-amino-5-chloro-2-phenyl-3-(2H)-pyridazinone, iso-PCA) and 4,5-dichloro-2-phenyl-3(2H)-pyridazin...

The possibility of NQ12 (2-chloro-3-[4-(ethylcarboxy)-phenyl]-amino-1,4-naphthoquinone) as a novel antithrombotic agent and its mode of action were investigated. The effects of NQ12 on platelet aggregation in human platelet-rich plasma in vitro, in rats ex vivo, and on murine pulmonary thrombosi...

The title compound 2-amino-8-chloro-4-phenyl-5,11-dihydro-6H-pyrido[2,3-a]carbazole-3-carbonitrile was prepared in good yield by multicomponent reaction under l-proline as promoter structure of the prepared compound was studied and characterized using IR, 1H and 13C NMR spectroscopic techniques....

Previously, we described alkoxyamines bearing a pyridine ring as new pro-drugs with low molecular weights and theranostic activity. Upon chemical stimulus, alkoxyamines undergo homolysis and release free radicals, which can, reportedly, enhance magnetic resonance imaging and trigger cancer cell ...

2,5-Dimethoxy-1,4-bis[2-(3,4,5-trimethoxyphenyl)ethenyl]benzene was synthesized using the Wittig reaction and the mixture of the three possible cis,trans-isomers was separated by preparative HPLC. The spectroscopy, conductivity and solubility of the isomers are presented. NMR measurements provid...

A series of novel N3/8-disubstituted-3,8-diazabicyclo[3.2.1]octanes in order to improve the in vitro activity of the prototype 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridyl-4-yl)methylpiperazine (1) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines. Compo...

A new series of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazoles were synthesized and their cytotoxic activities in vitro against four different cell lines (HT-29, MCF-7, NIH-3T3, AGS) were evaluated. Compound 6g bearing 3,4,5-trimethoxyphenyl moiety on ring A and 4-methoxy substituen...

The increase of the electrical conductivity of the arylenevinylene (AV) system 1,4-bis[2-(3,4,5-trimethoxyphenyl)ethenyl] benzene was measured as a function of the doping level of iodine. Compressed powders and films blended with polystyrene (PS) containing up to 30 wt.% of the oligomer were use...

Novel bioactive heterocycles containing a 3,4,5-trimethoxyphenyl fragment as antiproliferative agents by targeting tubulin were synthesized and their preliminary structure activity relationships (SARs) were explored. Among all these chemical agents, 2-(Benzo[d]oxazol-2-ylthio)-N-(4-methoxybenzyl...

N-{6-(Ferrocenyl) ethynyl-2-naphthoyl} amino acid and dipeptide ethyl esters 2–8 were prepared by coupling 6-(ferrocenyl) ethynyl-2-naphthoic acid 1 to the amino acid ethyl ester GABA(OEt) and the dipeptide ethyl esters GlyGly(OEt), GlyAla(OEt), SarGly(OEt), SarAla(OEt), ProGly(OEt) and ProAla(...

A stereodynamic chiroptical sensor based on three-component assembly of 3-(di-2-picolylaminoacetamido)-2-formyl-naphthalene (1), ZnII and amino acids was developed. The imine formed between 1 and an amino acid has six coordination sites to bind tightly ZnII ion. The crystal structure of the ZnII...

Treatment of 6-amino-2-naphthoic acid with dichlorotriphenylphosphorane afforded a new naphthalene ring-based calix[3]amide in moderate yield. The macrocyclic calix[3]amide exists in an anti-form in the crystalline state and forms a channel structure along its b axis. In CDCl3 solution it exists...