Photophysical properties of a bioactive flavonol which can be used as a model for polyhydroxylated natural flavonols, 3,6-diHydroxyflavone (3,6-diHF) in cyclodextrins (CDs)/bovine serum albumin (BSA) systems have been studied by absorption and fluorescence spectroscopy. The influence of CDs natu...
We have previously selected a promising anti-cancer agent 3,6-dihydroxyflavone by pharmacodynamic experiments. In the present study, we investigated its pro-apoptosis mechanisms in leukemia HL-60 cell. Our data revealed that 3,6-dihydroxyflavone dose- and time-dependently decreases cell viabilit...
4-aminophenyl-β-D-glucopyranoside has been electrochemically immobilized on carbon and PPF surfaces by oxidation of the amine. The unprotected glucoside layers were analyzed by XPS, AFM, CV and contact angle experiments. Results demonstrate that the carbohydrate-functionalized surfaces retain t...
The Electronic and Nonlinear Optical properties of the donor-acceptor molecules 2-(4-aminophenyl) Quinoline, 4-(4-aminophenyl) Quinoline, Anthraquinone; and the molecules Anthracene and Phenanthrene have been determined and some of these properties compared with literature values. The theoretica...
A facile electrooxidative method for synthesizing biaryls from arylboronic acids or arylboronic esters is described. In the presence of a catalytic amount of Pd(OAc)2 and TEMPO, the electrooxidation of arylboronic acids or arylboronates gave the corresponding biaryls in moderate to excellent yields.
An electrochemical method for generating cationic palladium complexes was integrated into an electrooxidative homo-coupling of arylboronic acids. In the presence of a catalytic amount of TEMPO, the homo-coupling reaction proceeded efficiently under argon to afford symmetric biaryls.
This chapter describes asymmetric reactions employing tartaric acid derivatives as chiral auxiliaries. The ready availability of both enantiomers and existence of four hydroxy groups were conducive to its use for asymmetric synthesis. The following article is basically focused on enantioselectiv...
Nitroso compounds are versatile reagents in synthetic organic chemistry. Herein, we disclose a feasible protocol for the ipso-nitrosation of aryl boronic acids using chlorotrimethylsilane–sodium nitrite unison as nitrosation reagent system.
The serotonin6 (5-HT6) receptor has received attention for its proposed role in cognitive impairments associated with schizophrenia and Alzheimer's disease. This has lead to a search for selective 5-HT6 receptor ligands useful for in vivo imaging in animals and humans. The novel 5-HT6 recep...
A novel, potent and selective quinazolinone series of inhibitors of p38α MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clinic...
A new series of 1-adamantyl derivatives was designed, synthesized and evaluated for their antimicrobial and antiviral activities. Representative derivatives of the newly synthesized compounds were tested. Ampicillin, clotimazole and the antiviral antibiotic aphidicolin were used as positive cont...
New 1-adamanyl-1,3,4-thiadiazole derivatives namely, 5-(1-adamantyl)-1,3,4-thiadiazoline-2-thione 3, 5-(1-adamantyl)-3-(benzyl- or 4-substituted benzyl)-1,3,4-thiadiazoline-2-thione 4a–d, 5-(1-adamantyl)-3-(4-substituted-1-piperazinylmethyl)-1,3,4-thiadiazoline-2-thiones 5a–c, 2-[5-(1-adamanty...
An efficient synthesis of 4-(1-adamantyl)benzoic acid based on transition metal ion catalyzed oxidation of 4-(1-adamantyl)toluene has been developed. As a catalytic system, cobalt–manganese bromide with addition of manganese acetate was used. A series of amino acid derivatives of 4-(1-adamantyl...
The oxime of 1-acetyl adamantane 2 is added to acetylene (KOH/DMSO, 70 °C, initial acetylene pressure 13 atm, 30 min) to afford the corresponding O-vinyl oxime 5 in 80% yield. The latter upon heating (DMSO, 120 °C, 1 h) gives 2-(1-adamantyl)pyrrole 3, 1-acetyl adamantane 1, and adamantane (6:3...
Novel 1-(2-aryl-2-adamantyl)piperazine derivatives have been synthesized and evaluated in vitro for their antitumor properties against HeLa cervical carcinoma, MDA MB 231 breast cancer, MIA PaCa2 pancreatic cancer, and NCI H1975 non-small cell lung cancer. The parent piperazine 6 was found to ex...
10-(Methoxyimino)phenanthren-9-one (1) reacts with DMAD (2) in dioxane to give dimethyl 7-oxo-7H-dibenzo[de,g]quinoline-4,5-dicarboxylate 4, whereas from the reaction of 1 with 2 in toluene besides 4, the oxazole 5 and also dimethyl 2-phenyldibenzo[f,h]-quinoline-3,4-dicarboxylate 6 are obtained...
7-Methoxyimino-4-methylchromene-2,8-dione 2 reacts with triarylphosphines 1(a-d) to give the unexpected 7-arylamino-8-hydroxy-4-methyl-2H-[1]-benzopyran-2-ones 7(a-d) and methyl diarylphosphinates 8(a-d) in high yields. The reaction of 2 with trialkylphosphines 1(e,f) as well as with diphenylpho...
A series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)-(methoxyimino)pentyl-1-piperazines was prepared and their affinity for the NK1 and NK2 receptors investigated. Compounds 7f, 10o, 10r, and 10s were found to be our most potent inhibitors.
7-Methoxyimino-4-methylchromene-2,8-dione 3, easily prepared from the quinone 1 reacts thermally with methylaromatics 5(a–g), benzyl derivatives 13(a–c), halo derivatives 14(a–c) to give mainly oxazolocoumarins. Products 8(a–d) are obtained from 5(a–d), 13(a–c). Compound 9 is obtained from...
A Z-isomer of 2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)acetic acid, which is the common acyl moiety of clinically useful cephalosporins, has been prepared from the aminoisoxazols through the thiadiazol-acetate in two pathways.
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