N-Substituted-2-amino-4(3H)-7H-oxopyrrolo[2,3-d]pyrimidine-5-carboxamides and their ribofuranosyl and 2′,3′-dideoxyribofuranosyl derivatives were prepared as membrane permeable echiguanine analogs and tested for their ability to inhibit phosphatidylinositol (PI) 4-kinase. Compounds 5 and 6 wer...

An efficient synthesis which utilizes a palladium catalyzed carbonylation reaction between 2-pivaloyl-7-iodo-7-deazaguanine and 3-aminopropionitrile as a key step was developed for the preparation of a new class of pyrrolopyrimidine based PI4-Kinase inhibitors: Echiguanines A and B.

The synthesis of ribofuranosyl glycosides of echiguanines A and B, PI 4-kinase inhibitors, was achieved from 2-amino-4-chloropyrrolo[2,3-d]pyrimidine and 2,3-O-isopropylidene-5-O-(t-butyl) dimethylsilyl-α-d-ribofuranosyl chloride. The ribofuranosyl echiguanine A weakly inhibited PI 4-kinase.

A new series of novel complexes of type cis-[Ru(CO)2Cl2(L)2], L = 2-phenyl-1,8-naphthyridine, 2-(4′-nitrophenyl)-1,8-naphthyridine, 2-(4′-bromophenyl)-1,8-naphthyridine, 2-(4′-methylphenyl)-1,8-naphthyridine, 2-(3′-methoxyphenyl)-1,8-naphthyridine, 2-(2′-methoxyphenyl)-1,8-naphthyridine and...

This study describes a simple and efficient procedure to synthesize a novel series of fourteen 4-substituted N-(5-pyridinyl-1H-1,2,4-triazol-3-yl)-6-(trifluoromethyl)pyrimidin-2-amines, where the 4-substituents are H, CH3, C6H5, 4-FC6H4, 4-CH3C6H4, 4-CH3OC6H4 and 2-Furyl; from the cyclocondensat...

Five neutral mononuclear copper(I) halide complexes containing 2,2,5,5-tetramethylimidazolidine-4-thione (tmimdtH) and triphenylphosphane (PPh3) or tri-o-tolylphosphane (totp) have been prepared and structurally characterized by X-ray single-crystal analysis. The complexes containing PPh3 adopt ...

Herein we report on the synthesis, molecular structures, DNA-binding properties and antibacterial activity of four new copper(I) mixed-ligand complexes obtained by reacting copper(I) halides or [Cu(CH3CN)4](BF4) with 1,2-bis(diphenylphosphano)ethane (dppe) and 2,2,5,5-tetramethylimidazolidine-4-...

A systematic synthesis of the N-methyl-1-deoxynojirimycin-containing oligosaccharides related to the Lewis x, Lewis a, sialyl-Lewis x and sialyl-Lewis a antigens has been achieved. The couplings of the suitably protected 1-deoxynojirimycin derivative 10 with methyl-1-thioglycosides (glycosyl don...

Human blood group A, B, H, Ii, Lea and Leb antigens and their determinants expressed on ovarian cyst glycoproteins have been studied for over five decades. However, little is known about sialyl Lex and sialyl Lea glycotopes, which play essential roles in normal immunity, inflammation, and cancer...

β-Enaminals were successfully synthesized in good to excellent yields by the reaction of C2-formylglycals with primary amines. Subsequent reaction with NaBH4 in HOAc led to unexpected reductive cleavage of allyl ether, i.e., the hydrodealkoxylation took place to produce the corresponding 3-deox...

A simple protocol is described for the synthesis of 2-(trifluoromethyl)benzo[b][1,8]naphthyridin-4(1H)-one derivatives. The reaction between diverse 2-chloro-3-acetyl-quinolines with trifluoroacetimidoyl chlorides using sodium hydride in THF at room temperature gives directly the title compounds...

A new approach to arylated 2-trifluoromethylquinolines based on novel regioselective Suzuki-Miyaura coupling reactions has been developed. Moreover, site-selective, chemo-selective amination reactions were performed. The new 2-trifluoromethylquinoline derivatives were tested as potential NPPs in...

A novel series of 4-alkynyl-quinoline derivatives were designed, synthesized and biologically evaluated for their PI3Kα inhibitory activities and anti-proliferative effects against two cancer cell lines PC-3 and HCT-116. Most of them showed potent PI3Kα inhibitory activities with IC50 values a...

The gold-catalyzed Friedlander reaction was applied to the condensation of 2-aminoarylketones with β-keto-esters, β-diketones, β-keto-amides, and β-keto-sulfones to afford a diverse range of 2,3,4-trisubstituted quinolines in 3–82% yield. The seven-membered rings 1,3-cycloheptadione and aze...

Screening a compound library of quinolinone derivatives identified compound 11a as a new P2X7 receptor antagonist. To optimize its activity, we assessed structure-activity relationships (SAR) at three different positions, R1, R2 and R3, of the quinolinone scaffold. SAR analysis suggested that a ...

We present syntheses, prediction of tautomer forms and activities of the second generation of the Mdm2-p53 inhibitors that are based on the tetramic acid scaffold. The inhibitors do not contain 6-chloroindole. Binding of these compounds to Mdm2 was checked by two orthogonal methods: the fluoresc...

To discover more derivatives with better glucose-lowering efficacy compared with berberine, twenty-three novel compounds with 4,7,12,12a-tetrahydro-5H-thieno[3′,2′:3,4]pyrido[1,2-b]isoquinoline or 5,8,12,12a-tetrahydro-6H-thieno[2′,3′:4,5]pyrido[2,1-a]isoquinoline cores were designed, synthe...

The paper presents a combined experimental and computational study for three oxalate copper(II) complexes [Cu(ptz)2(C2O4)(H2O)]·1.5H2O (1), [Cu(dppt)(C2O4)(H2O)]·H2O·MeOH (2) and [Cu(dmdpq)(C2O4)(H2O)]·5H2O (3) (ptz = phthalazine, dppt = 3-(2-pyridyl)-5,6-diphenyl-1,2,4-triazine and dmdpq = ...

2-Amino-5,6-dimethyl-1,2,4-triazine (ADMT) reacts instantaneously with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) in acetonitrile (AN) forming reddish brown charge transfer complex. Absorption spectra of the complex produced multi-charge transfer bands at 460, 560 and 589 nm, respectively. Th...

With the purpose of studying the binding behavior of Pd(II) complexes with DNA as the main biological target, and their ability to penetrate reasonably into tumour cells and destroy their replication ability, Pd(ADT)Cl2 complex was synthesized and characterized, where ADT is 3-amino-5,6-dimethyl...