Background: Angiogenesis, the formation of new blood vessels, is essential for tumor growth. The inhibition of angiogenesis is therefore emerging as a promising therapy for cancer. Two natural products, fumagillin and ovalicin, were discovered to be potent inhibitors of angiogenesis due to their...

Total syntheses of (±)-ovalicin, its C4(S∗)-isomer 44, and C5-side chain intermediate 46 were accomplished via an intramolecular Heck reaction of (Z)-3-(tert-butyldimethylsilyloxy)-1-iodo-1,6-heptadiene and a catalytic amount of palladium acetate. Subsequent epoxidation, dihydroxylation, methyl...

This review covers comprehensively the authors work during the present decade based on the chemistry of ionic organometallic hydrazines formulated as [(η5-Cp′)Fe(η6-Ar-NHNH2)]+PF6− (Cp′ = C5H5, C5Me5; Ar = aryl), that could be considered as a new generation of hydrazines owing to the changes...

Various trialkylchlorosilanes were reacted with a number of molybdenum-oxo complexes in order to establish the main factors which influence the process of addition of the SiCl function across the MoO bond. A novel intermolecular mode of hexaalkyldisiloxane formation was observed in one case.

Protonation constants of oxalate (ox2-) were obtained, by potentiometric measurements, in NaCl, KCl and tetraethylammonium iodide aqueous solutions in the ranges 5 ⩽ T ⩽ 50°C and 0 ⩽ I ⩽ 1 mol dm−3. The differences in protonation constant values were explained by a complex formation model assum...

The reducing action of some aliphatic and aromatic hydrocarbon derivatives on the oxides of Me, W, Ti, Zr, Nb and Ta was compared to that of graphite powder. The investigation showed that among the organic compounds studied tetraethylammonium iodide gives a better separation of the volatile elem...

The protonation of 2- and 3-nitrophenol (NO2 Ph) and 2,X and 3,Y dihydroxybenzoic acids (DBA, X = 4,5,6; Y = 4,5) has been studied potentiometrically in aqueous tetraethylammonium iodide solutions, at T = 25° in the ionic strength range 0.05:5 ≤ I ≤ 1M. Besides the species reported in the lit...

An efficient approach to aryl azides, in short reaction times and good to excellent yields, has been developed via the reaction of aryl halides with sodium azide under Cu2O/tetraethylammonium prolinate catalysis.

The data regarding the protonation of 22-(mono-, di-,…, penta-) carboxylic acids in aqueous tetraethylammonium iodide at different ionic strengths 0

The interactions of amino acids glycine, l-alanine and l-valine with tetraethylammonium iodide (TEAI) as a function of temperature have been investigated by a combination of volumetric and acoustic measurement. Densities (ρ) and ultrasonic speeds (u) of amino acids in aqueous solutions of TEAI ...

Knowledge of thermodynamic properties of substituted amino acids in aqueous medium can provide valuable information regarding the stabilisation mechanism of proteins. In this study, we report the density and ultrasonic speeds of N-acetyl glycine in (0.03, 0.05, 0.1, 0.15 and 0.2) mol ⋅ kg−1 aque...

Viscosities, η, for solutions of glycine, l-alanine and l-valine in (0.03, 0.05, 0.1, 0.15 and 0.2) mol·kg− 1 aqueous tetraethylammonium iodide (TEAI) at temperature T = (288.15, 293.15, 298.15, 303.15 and 308.15) K have been measured as a function of molality of amino acids. The viscosity B-c...

2-Carbomethoxycyclobutanone reacted with N-phenyl-C-arylnitrones to afford methyl 5-oxo-2-[aryl(phenylamino)methyl]tetrahydrofuran-2-carboxylates by the catalysis of indium(III) triflate in the presence of magnesium sulfate.

Hybridization strategy is an effective strategy to obtain multi-target inhibitors in drug design. In this study, we assembled the pharmacophores of momelotinib and tandutinib to get a series of 4-piperazinyl-2-aminopyrimidine derivatives. All compounds were tested for the inhibition of JAK2 and ...

Two tetrahydrofuran-based γ-amino acids [2,4-cis and 2,4-trans] were subjected to iterative peptide-coupling procedures to afford dimeric, tetrameric and hexameric carbopeptoids in good yield. These homooligomers were prepared for secondary structural study—to ascertain the conformational pref...

Voltage-gated sodium channels play an integral part in neurotransmission and their dysfunction is frequently a cause of various neurological disorders. On the basis of the structure of marine alkaloid clathrodin, twenty eight new analogs were designed, synthesized and tested for their ability to...

Using 21 newly synthesized 7,7′-dioxo-9,9′-epoxylignane derivatives having a modified 7-phenyl group, we examined the relationship between their structure and antifungal activity against plant pathogens such as Bipolaris oryzae to determine the effects of various substituents on the antifungal...

cis-3-Benzyloxy-4-(2-mesyloxyethyl)azetidin-2-ones were shown to be useful starting products for the synthesis of cis-2-oxa-6-azabicyclo[3.2.0]heptan-7-ones in high overall yields and purity upon hydrogenolysis of the benzyl ether substituent followed by intramolecular nucleophilic substitution ...

Phenyl cations are short-lived electrophiles and can be smoothly generated by photolysis of aromatic halides (chlorides, fluorides) and esters (sulfonates, sulfates and phosphates) in protic media. Indeed, the heterolytic cleavage of an ArylLG bond (LG = leaving group; X, OR) allows for the gene...

2,4-Disubstituted phenyl 10-methyl-10λ4-acridine-9-carboxylate derivatives were synthesized and the chemiluminescence of each was measured at pH 6–9. The introduction of electron-withdrawing groups at 2,4-positions in the phenyl moiety intensified chemiluminescence. 2,4-(Dimethoxycarbonyl)phen...