Pancreatic cancer is one of the most lethal of human malignancies. Nearly 100% cases of pancreatic cancer carry mutations in KRas. P-21-activated kinases (PAKs) are activated by and act downstream of KRas. Glaucarubinone, a natural product first isolated from the seeds of the tree Simarouba glau...
Crystalline materials from a high-boiling fraction obtained as by-products in the preparation of C6F5AsCl2, or from subsequent reaction with elemental mercury, have been crystallographically identified as consisting primarily of secondary and tertiary substituted pentafluorophenylarsenic compoun...
Tris(pentafluorophenyl)-substituted pnictogenes (excluding nitrogen) are able to arylate electrophilic compounds containing active halogen atoms in the presence of CsF in bipolar aprotonic solvents.
The reactions of tris(pentafluorophenyl)arsenic(III) with iodine monochloride, iodine monoazide, and dithiocyanogen yielded corresponding oxidative-addition products of the type (C6F5)3As(V)XY (X=I, Y=Cl, N3; X=Y=NCS). The elemental sulphur also added oxidatively with tris(pentafluorophenyl)arse...
Tris(pentafluorophenyl)phosphine is oxidised by bis(trifluoromethyl)nitroxyl to form tris(pentafluorophenyl)phosphine oxide and perfluoro(2,4-dimethyl-3-oxa-2,4-diazapentane). With the corresponding arsine and stibine, addition products are obtained, namely tris(pentafluorophenyl)-arsenicdi[bis(...
Excess molar volumes, VEm, were measured as a function of mole fraction at 298.15 K and atmospheric pressure for the seven mixtures (chloro- or methylcyclohexane + ethanol or propan-1-ol or propan-2-ol and chlorocyclohexane + methanol). The results are compared with VEm values for cyclohexane + ...
The enthalpies of solution at infinite dilution of 2-chloro-2-methylpropane in 9 dialcohols and of 2-chloro-2-methylbutane and 3-chloro-3-methylpentane in 19 mono- and dialcohols, at 298.15 K, were measured using a solution calorimeter. These values are discussed in terms of solute-solvent inter...
The solubility of 3-chloro-N-phenylphthalimide in acetonitrile, methanol, n-propanol, isopropanol, n-butanol, 2-methyl-1-propanol, ethyl acetate, acetone, 1,4-dioxane and acetic acid were obtained experimentally with the high-performance liquid chromatography analysis at temperature ranging from...
Solubilities of 5-chloro-1-methyl-4-nitroimidazole in eleven organic solvents of methanol, ethanol, isopropanol, n-propanol, N-methyl-2-pyrrolidone, ethyl acetate, toluene, acetone, 2-butanone, trichloromethane and 1,4-dioxane were measured by using an isothermal saturation method at temperature...
The neuroleptic drug thioridazine has been recently repositioned as possible anti-tubercular drug. Thioridazine showed anti-tubercular activity against drug resistant mycobacteria but it is endowed with adverse side effects. A small library of thioridazine derivatives has been designed through t...
SummaryThioridazine, a potent phenothiazine compound was evaluated for its chemotherapeutic efficacy against experiment model of tuberculosis. Thioridazine potentiated the activities of both isoniazid and rifampicin (>1 log CFU reduction) against the in vitro latent Mycobacterium tuberculosis ba...
In this paper, we describe the direct, preparative enantioselective chromatography of racemic (rac)-propranolol hydrochloride (HCl) and rac-thioridazine·HCl using Chiralpak AD chiral stationary phase and mobile phase systems containing carbon dioxide and methanol without the use of basic or aci...
Thioridazine is an orally administered antipsychotic drug with potential for treatment of drug-resistant tuberculosis (TB). However, drug-induced adverse cardiac effects have been reported when thioridazine was used at an efficacious oral dose of 200 mg/day to treat TB. Pulmonary delivery of thi...
Publisher SummaryThis chapter discusses the analytical profile of thioridazine hydrochloride. Thioridazine is commercially available as the base and as the hydrochloride salt. Thioridazine and its HC1-salt are white to slightly yellow crystalline powder with a faint odor and a very bitter taste....
Hydrogen peroxide, potassium permanganate, potassium dichromate, potassium hexacyanoferrate(III), cerium(IV) sulphate and sodium peroxidisulphate have been tested as potential reagents for chemiluminescence generation from the oxidation of phenothiazine derivatives. Only with potassium permangan...
A simple, sensitive and specific fluorimetric method has been developed for the determination of thioridazine hydrochloride in human plasma involving solid phase extraction (SPE). In a flow-injection system, thioridazine hydrochloride is on-line oxidized into a strongly fluorescent compound with...
Applications of quantitative structure-activity relationship (QSAR) procedures to our own practical drug research are reviewed. A benzylpiperazine cerebral vasodilator (KB-2796) and a piperazine-acetate antiulcer agent (KB-5492) were successfully optimized by use of QSAR information. In these ca...
A simple biologically active phenolic methyl gallate (MeG) was used as a model compound to identify the nature of the complexes it formed with Al3+, Fe3+, Cu2+, and Sn2+ as analyzed by ultraviolet (UV) spectroscopic and computational methods. The results showed that, among all the metal ions stu...
Palmitoyl-epigallocatechin gallate (p-EGCG), a palmitic acid ester derivative of epigallocatechin gallate (EGCG), has been declared with high bioactivity. Synthesis of p-EGCG with microwave irradiation as well as its antioxidant activity by Rancimat test was investigated in this study. With micr...
In real flotation systems, the flotation separation of fluorite from calcite is a challenge due to the similar surface properties of these two minerals. The purpose of this paper is to develop a highly selective flotation collector for the separation. Propyl gallate (PG) was introduced as a coll...
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