A series of new 2,4-diarylaminopyrimidine analogues (DAAPalogues) was developed by incorporation of a substituted 2-aminothiazole component as the C-2 substituent of the center pyrimidine core. Compound 5i showed highest potency of 12.4 nM against ALK and 24.1 nM against ALK gatekeeper mutation ...

A series of compounds 4-oxo-thiazolidine derivatives AJ5a–j were synthesized by condensation reactions. The structure of synthesized compounds was characterized by IR, 1H NMR, 13C NMR and mass spectroscopy. The present paper deals with newly synthesized thiazolidine compounds AJ5a–AJ5j that we...

With an intention to synergize the anti-bacterial activity of chalcones and rhodanine-3-acetic acid, several hybrid compounds possessing chalcone and rhodanine-3-acetic acid moieties were synthesized and tested for their anti-bacterial activity. Some compounds presented great anti-microbial acti...

Oxovanadium(IV)-catalyzed oxidation of substituted 4-oxo-4-phenyl-butanoic acids (4-oxo acids) by bromate in acid medium leads to the formation of malonic acid and the corresponding benzoic acid. The reaction exhibits first order each in [bromate] and [acid], less than unity order each in [4-oxo...

Protonation of the reactive intermediates produced in the reaction between tert-butyl isocyanide and dialkyl acetylenedicarboxylates by aromatic carboxylic acids leads to vinylnitrilium cations, which undergo nucleophilic reaction with conjugate bases of the carboxylic acids to produce dialkyl (...

Oral drug administration remains the preferred approach for treatment of HIV in most patients. Maraviroc (MVC) is the first in class co-receptor antagonist, which blocks HIV entry into host cells. MVC has an oral bioavailability of approximately 33%, which is limited by poor permeability as well...

We have measured the Compton profiles (CP's) or the isomers: methyl formate and acetic acid using 59.54 keV γ-rays from a241 Am source and a Si(Li) detector. The measured profiles are compared with theoretical calculations based on Epstein's localized molecular orbital (LMO) calculati...

During the investigation of antagonists for the MC4 receptor, we found that 10ab having a naphthyl group showed almost the same binding affinity for the MC4 receptor as that of the lead compound 1 with a benzoyl group. We also developed a new type of compounds, namely, bis-piperazines, and found...

A series of 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine derivatives were synthesized. In initial screening and quantitative evaluation, compound 2r was among the most active agents, exhibiting in the same time the lowest toxicity. In the anti-maximal electroshock test, it showed median effective d...

A new series of tacrine-based acetylcholinesterase (AChE) inhibitors 7a–l were designed by replacing the benzene ring of tacrine with aryl-dihydropyrano[2,3-c]pyrazole. The poly-functionalized hybrid molecules 7a–l were efficiently synthesized through multi-component reaction and subsequent Fr...

Few investigations have been made to apply thermal analysis methods on solid residue analysis to understand biomass liquefaction mechanistic information. To investigate the mechanism of cornstalk liquefaction in water/ethanol mixtures, the solid residues remaining after the liquefaction process ...

Antioxidant defense is crucial in restoring cellular redox homeostasis. Recent findings have suggested that oxidative stress plays pivotal roles in the pathogenesis of many neurodegenerative diseases. Thus, an anti-oxidative stress remedy might be a promising means for the treatment of such diso...

Carbonothioic O,O-acid (monothiocarbonic acid), the sulfur analogue of carbonic acid, is thus far an experimentally unreported molecule of atmospheric and biochemical relevance. Computations at the CCSD(T)/cc-pVQZ//CCSD(T)/cc-pVTZ level of theory reveal that its carbonothioic O,S-acid tautomer i...

Transparent Barium Bismuth Borate glasses are synthesised with melt-quenching technique. The linear properties of the glasses are studied with UV–Vis absorption studies. Raman spectra was used to study the structural units of the BBB glasses. Linear absorption, optical band gap and Raman spectr...

Both histone deacetylase (HDAC) and fibroblast growth factor receptor (FGFR) are important targets for cancer therapy. Although combining dual HDAC pharmacophore with tyrosine kinase inhibitors (TKIs) had achieved a successful progress, dual HDAC/FGFR1 inhibitors haven’t been reported yet. Here...

Oxidation of 1-methylcyclobutene (1) by PdCl2L2 and PdCl(NO2)L2 (LCD3CN) in methylene chloride was studied with 1H and 13C NMR. Reaction of 1 with PdCl2L2 leads to the formation of the stable ring-opened 1-3-η3-π-allyl palladium complex (2). With the addition of an equimolar quantity of PdCl...

The monomer, 1-methylcyclobutene I can be polymerized by a number of well-defined alkylidene complexes of the type M(CH(CH3)2R)(NAr) (OC(CH3)itn (CF3)3-n)2 (where Ar = 2,6-diisopropylphenyl) to give highly stereoregular polyisoprenes. Only II (where M = Mo; R = Ph; n = 2) catalyzes the polymeriz...

The application of 4-[(4-methylphenyl)sulfonyl]-1-(triphenylphosphoranylidene)-2-butanone, a readily available four-carbon building block, to the synthesis of 3-deoxy-d-manno-2-octulosonic acid (KDO) is described.

The herein synthesized 7-(4-methylphenyl)thiomethyl and 7-morpholylmethyl derivatives of natural phaeosphaeride A have lower cytotoxic activity towards the human lung adenocarcinoma A549 cell line compared to phaeosphaeride A. The presence of exocyclic C=C bond and N–OMe group in such compounds...

Asymmetric synthesis of four novel C-nucleosides, (2′R,5′R)-, (2′S,5′R)-, (2′S,5′S)- and (2′R,5′S)-2-[2-hydroxymelhy])-1,3-dioxolan-5-yl]-1 ,3-thiazole-4-carboxamide has been accomplished by the condensation of key intermediates, 2-(1R- and 1S-glycol-1-yl)-4-ethoxycarbonyl-1,3-thiazole w...