Small molecules that target microtubules (MTs) represent promising therapeutics to treat certain types of cancer, including glioblastoma multiform (GBM). We synthesized modified carbazoles and evaluated their antitumor activity in GBM cells in culture. Modified carbazoles with an ethyl moiety li...

A Suzuki-Miyaura cross coupling, followed by triphenylphosphine mediated Cadogan reductive cyclization sequence provided efficient access to a series of carbazole alkaloids.In the present work, this approach was applied to the total synthesis of mukonine, clauszoline K, koenoline, murrayanine, m...

Four new carbazole-based coumarin derivatives comprising a carbazole core and one or two coumarin chromophores, 7-(diethylamino)-3-(4-(9-(p-tolyl)-9H-carbazol-3-yl)phenyl)coumarin (Cz-Ph-C) and 3,3'-((9-(p-tolyl)-9H-carbazole-3,6-diyl)bis(4,4′-phenyl))bis(7- (diethylamino)coumarin) (Cz-2(P...

The compound 9-p-tolyl-9H-carbazole-3-carbaldehyde (HCCD) was synthesized and characterized by X-ray diffraction, FT-IR, FT-Raman and UV–Vis spectra. The X-ray diffraction study showed that HCCD has a Z-configuration. The benzene ring including methyl is twisted from the mean plane of the carba...

An efficient copper-catalyzed double C–N bond forming reaction using diiodides and nitrogen-centered nucleophiles including amides and carbamates is reported. The reactions proceed to afford di- or tri-substituted N-acylpyrroles, dihydropyrroles, and carbazoles in good to excellent yields when ...

A SAR study on derivatives of 2-amino-1-benzyl-4,5-diphenyl-1H-pyrrole-3-carbonitrile 5a revealed that the 3-carbonitrile group, vicinal 4,5-diphenyl and N-benzyl side chains of the pyrrole are important for the inhibitory potencies of these compounds against members representing the three main ...

(2,4-Dimethoxybenzyl)hydrazine (DmbNHNH2) was utilized in the synthesis of Dmb-protected 4-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenols. This unambiguous protection of the pyrazole endocyclic nitrogen atom enabled the preparation of amino-substituted 4-((3,5-diamino-1H-pyrazol-4yl)diazenyl)phe...

In this study, a series of novel thiazolidin-4-ones (5a–g) and azetidin-2-ones (6a–g) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl)hydrazine carboxamide derivatives of the benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gra...

Neuropathic pain is a chronic pain condition that occurs and persists in a heterogeneous group of etiologically different diseases characterized by a primary lesion or dysfunction of the peripheral or central nervous system. Current treatment options do not provide adequate relief for many patie...

The 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging assay was used to determine the antioxidant activity of novel 3-benzylidene-3-methyl-2,6-diarylpiperidin-4-ones, which were efficiently synthesized in the presence of an eco-friendly montmorillonite-KSF clay catalyst. The synthesized compounds ...

A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5 were synthesized from 2-amino-4-arylthiazoles 1 and 2-chloro-acetamido-4-arylthiazoles 2 via th...

Cadmium is a heavy metal present in contaminated soils. It has no biological role but when entering cells generates DNA damage, overexpression of stress response proteins and misfolded proteins, amongst other deleterious effects. Acidithiobacillus ferrooxidans is an acidophilic bacterium resisti...

Heavy metal tolerance of microorganisms is the basis of heavy metal removal by growing cells. In this study, a cross-protection effect generated by salt stress significantly enhanced the cadmium tolerance of multi-stress-tolerant Pichia kudriavzevii. Comparative transcriptome analysis using RNA-...

A Mo(III) cadmium diphosphate, Cd5Mo2(P2O7)4 has been synthesized for the first time. Its structure determination shows that the crystal chemistry of this new monoclinic phosphate is complex, due to the ability of cadmium to behave either as an interpolated cation, or as a building unit for the ...

The properties of poly(oxyethylene) dicarboxylic (POEDC) and diphosphoric (POEDP) acids as macromolecular carriers (macroionophores) of metal cations have been investigated and compared to the properties of poly(ethylene glycol)s. The macroionophores were dissolved in 1,2-dichloroethane forming ...

An enantioselective gas chromatographic quantitation assay was developed for the enantiomers of dl-threo-methylphenidate in plasma and urine. dl-threo-Methylphenidate and the internal standard were acylated with N-heptafluorobutyryl-1-prolylchloride under Schotten—Baumann conditions prior to ga...

BackgroundFatigue is a common complaint in patients with sarcoidosis. We studied the effectiveness of dexmethylphenidate hydrochloride (d-MPH) in treating sarcoidosis-associated fatigue.

The regional distribution of [11C]d-threo-methylphenidate in mouse brain was very similar to that of [3H]WIN 35,428 ((−)-2β-carbomethoxy-3β-(4-fluorophenyl)tropane), and the two radioligands were displaced from striatum similarly after administration of the potent cocaine analog RTI-55 ((−)-2β...

ABSTRACTObjective:To evaluate the efficacy and safety of dexmethylphenidate hydrochloride (d-MPH, Focalin™) for the treatment of attention-deficit/hyperactivity disorder (ADHD) and to test an a priori hypothesis that d-MPH would have a longer duration of action than d,l-threo-methylphenidate (d,...

ABSTRACTObjective:Methylphenidate has four optical isomers due to two asymmetries (erythro-threo and dextro-levo). The initial commercial formulation eliminated the erythro isomer, but the dextro-levo asymmetry was racemic, with equal amounts of d and l-threo isomers (d,l-MPH). Previous work has...