We designed new 3-arylthio- and 3-aroyl-1H-indole derivatives 3–22 bearing a heterocyclic ring at position 5, 6 or 7 of the indole nucleus. The 6- and 7-heterocyclyl-1H-indoles showed potent inhibition of tubulin polymerization, binding of colchicine to tubulin and growth of MCF-7 cancer cells....

Bcl-2 proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, has been implicated in the progression and survival of multiple tumor types and become a validated and attractive target for cancer therapy. In this work, a series of 1-phenyl-1H-indole der...

A new series of N’-(substituted phenyl)-5-chloro/iodo-3-phenyl-1H-indole-2-carbohydrazide (5, 6) and N-[2-(substituted phenyl)-4-oxo-1,3-thiazolidin-3-yl]-5-iodo/chloro-3-phenyl-1H-indole-2-carboxamide (7, 8) derivatives were synthesized and evaluated for their anticancer properties. Compounds ...

3-Sulfonyl and 3-aroylindoles have attracted special attention because of their interesting biological activities, particularly for the development of antiviral and anticancer compounds. Based on the importance of the trifluoromethyl group in biological active molecules, we have developed a synt...

Excimer formation from 1-pyrenemethanol (PyM) and several other pyrene derivatives is investigated in aqueous dispersions of polystyrene (PS) latex, as well as in homogeneous solutions. The efficiency of excimer formation is markedly enhanced on going from the homogeneous aqueous solutions to th...

Photoinduced electron transfer from indolic compounds to 1-pyrenemethanol (PyM) in polystyrene latex dispersions has been studied by steady-state and time-resolved fluorescence spectroscopy. The photoinduced electron transfer reaction is observed by monitoring fluorescence quenching of PyM. The ...

A series of 21 novel N1-(2-aryl-1,3-thiazolidin-4-one)-N3-aryl urea derivatives based on the previously identified lead compound I were synthesized and biologically characterized. The most promising compound 19a was identified as a multi-tyrosine kinase inhibitor, including c-Met, Ron, c-Kit, AX...

The objective of this work was to assess the effect of surfactants and oils of a commercial formulation on the potential mobility of penconazole in agricultural soils that have been subjected to a high rate of application of agricultural chemicals. Soil–water partition tests on a commercial wat...

Drought stress is one of the most important environmental factors that limit plant growth. Canola is an important agricultural crop grown primarily for its edible oil. In this study, penconazole (PEN), a triazole growth regulator, and calcium (Ca2+), a secondary messenger, were used to analyses ...

This study investigated the effects of sugarcane bagasse compost (SBC) and chicken manure compost (CMC) on the sorption–desorption, leaching and bioavailability of the fungicide penconazole in soil in a laboratory setting. The autoclave-treated SBC or CMC was applied at 2.5% and 5.0% (w/w). Res...

Endocrine disruptive compounds are widely used and well-known chemicals that could alter some vital processes taking place in living organisms. These chemicals might cause serious health disorders such as different types of cancer, sexual anorexia and mood disorders. In this study, combination o...

Penconazole is a systemic triazole fungicide mainly used on grapes. The UE Maximum Residue Level (MRL) for penconazole is set at 0.2 ppm in wine and grapes. In the aim of identifying potential biomarkers of exposure to penconazole and possibly highlighting its endocrine disrupting mode of action...

Penconazole (PEN) and tebuconazole (TEB) are fungicides widely used in vineyards. The aim of this the study was to assess the suitability of hair to assess long-term exposure to PEN and TEB.Hair samples of agricultural workers exposed to PEN (AW-PEN, 18 subjects) or TEB (AW-TEB, 2 subjects) duri...

Penconazole (PEN) is a fungicide used in agriculture. The aim of this work was to evaluate the exposure to PEN in vineyard workers focusing on urinary biomarkers.Twenty-two agricultural workers were involved in the study; they were investigated during PEN applications and re-entry work, performe...

The present study pertains to the possible adverse effects of penconazole exposure on the lung of adult rats, and to the potential ability of vitamin E (Vit E) in mitigating the toxicity induced by this fungicide. Male Wistar rats were divided into four groups of six animals each: Group I (Contr...

Penconazole is a typical triazole fungicide with wide use on fruits, vegetables, and tea plants to control powdery mildew. In the present study, an efficient graphite carbon black solid phase extraction (GCB-SPE) purification combined with chiral ultra performance liquid chromatography tandem ma...

Penconazole is a widely used fungicide that is toxic to a variety of organisms including fish. In the present study, we investigated the developmental toxicity of penconazole on zebrafish embryos by exposing to different concentrations of penconazole (0.8, 1.6 and 2.4 mg/L) from 4-h post-fertili...

An efficient and large scale preparation of (2R,2′R)-(+)-threo-methylphenidate hydrochloride (3) by the resolution of (±)-threo-methylphenidate hydrochloride (1) salt with O,O′-dibenzoyl-d-(+)-tartaric acid in the presence of 4-methylmorpholine is described.

The 1:1 and 2:1 complexes of N-methylmorpholine betaine (MMB) with picric acid (TNPH) have been prepared and their structures determined by X-ray diffraction. In the 1:1 complex, MMBH·TNP, betaine is protonated and carboxylate group forms a hydrogen bond with the picrate anion, the O⋯O distance...

Fourteen complexes of N-methylmorpholine betaine (MMBet) with phenols (pKa from 9.99 to 0.33) are synthesized and analysed by 1H and 13C NMR in DMSO-d6 and UV–Vis spectroscopy in CH2Cl2, CH3CN and DMSO. The UV spectra of complexes with medium-strong phenols show separate absorptions for A–H⋯B ...