Benzyl trifluoromethyl ketone and ethyl bromoacetate afforded ethyl 3-hydroxy-4-pheny1-3-(trifluoromethyl)butanoate in a Reformatskytype reaction. This hydroxy ester, by successive stages of dehydration to a but-2-enoate, hydrogenation of the double bond, nitration, and conversion of the nitro g...

Preclinical investigations and early clinical trial studies suggest that FLT3 inhibitors offer a viable therapy for acute myeloid leukemia. However, early clinical data for direct FLT3 inhibitors provided only modest results because of the failure to fully inhibit FLT3. We have designed and synt...

Inspired by that the multi-target inhibitors against receptor tyrosine kinases (RTKs) have significantly improved the effect of clinical treatment for cancer, and based on the chemical structure of Linifanib (ABT-869, Abbott), two series of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino...

There is still a great demand in the clinic for the drugs which can overcome a variety of imatinib resistant ABL mutants. Starting from a type I inhibitor axitinib, which has been reported to overcome ABL-T315I mutant induced resistance, through a structure guided drug design approach and bindin...

The synthesis and anticonvulsant properties of new N-Mannich bases of 3-phenyl- (9a–d), 3-(2-chlorophenyl)- (10a–d), 3-(3-chlorophenyl)- (11a–d) and 3-(4-chlorophenyl)-pyrrolidine-2,5-diones (12a–d) were described. The key synthetic strategies involve the formation of 3-substituted pyrrolidi...

The main objective of the present work was to modify multiwalled carbon nanotubes (MWCNTs) using 3-aminopropyl-triethoxysilane (APTES) to generate amino-terminated surfaces for inulinase immobilization, which can be further used for fructose production. CCRD of response surface methodology was u...

Polyvinyl alcohol nanocomposite containing immobilized [Mn(Br4TPP)OAc] complex on bio inspired copper oxide was prepared by an electrospinning method ([email protected]). This novel heterogeneous biocatalyst based on Carthamus tinctorius plant was characterized by TEM, SEM, AFM, EDAX, elemental ...

In the present work, the gas-phase standard molar enthalpy of formation of 2-(1H-indol-3-yl)ethanol was derived, at T = 298.15 K, from the enthalpy of combustion for the crystalline compound, measured by static-bomb calorimetry, and its enthalpy of sublimation obtained from Calvet microcalorimet...

A cyclodextrin-modified micellar electrokinetic chromatography (CD-MEKC) method with hydroxypropyl-γ-cyclodextrin (HP-γ-CD) as chiral selector for the enantiomeric separation of econazole is reported. Enantioseparation of econazole was successfully achieved by the optimized CD-MEKC system cont...

Here we report the preparation of a trimethoprim/2-hydroxypropyl-γ-cyclodextrin inclusion complex along with a physicochemical study, structural characterization, and molecular modeling of the complex. As main results, we observed from phase-solubility studies at two temperatures (20 °C and 35...

Herein we report the formation of dry powder complexes of ibuprofen (IBU) and hydroxypropyl-γ-cyclodextrin (HP-γ-CyD) by supercritical CO2-assisted spray-drying (SASD). SASD of HP-γ-CyD alone, IBU/HP-γ-CyD, as well as the physical mixture were prepared and characterized using attenuated tota...

Curcumin is one of promising agents to accelerate the wound-healing process. However, the efficacy of curcumin is limited due to its poor water solubility and stability. To enhance the properties of curcumin, 2-hydroxypropyl-γ-cyclodextrin (HP-γ-CyD) can be used through complexation. Recently,...

Atrazine (ATZ) and ametryne (AME) inclusion complexes with 2-hydroxypropyl-β/γ-cyclodextrin (2-HP-β/γ-CD) in aqueous media and solid state were studied. Electrospray ionization mass spectrometry (ESI-MS), 1D (1H), and 2 D (DOSY, ROESY) nuclear magnetic resonance spectroscopy (NMR) were utili...

In this study, we investigated curcumin (CUR) solubility profiles and hydration/desolvation effects of this substance formulated with γ-cyclodextrin (γ-CD) and hydroxypropyl-γ-cyclodextrin (HP-γ-CD) excipients. The CUR/HP-γ-CD complex was found to be more stable in solution with the highest...

The inclusion complexes of imazapyr (IMA) with 2-hydroxypropyl(β/γ) cyclodextrins (HP β/γ-CD), have been studied in aqueous media and in the solid state. In this work, fluorescence spectroscopy, electrospray-ionization mass spectrometry (ESI-MS), and 1HNMR were used to investigate and charac...

We have measured the proton spin-lattice relaxation rate as a function of temperature in polycrystalline 3-ethylchrysene at nuclear magnetic resonance Larmor frequencies of 53.0 and 22.5 MHz and in polycrystalline 3-isopropylchrysene at 53.0, 22.5 and 8.50 MHz. The syntheses of these new compoun...

N-[(4-bromo-3,5-difluorine)phenyl]acrylamide is a new monomer for polymerization reactions. Information on its corresponding solid–liquid equilibrium is essential for industrial product and process design. Using a laser detecting system, solubility data were measured for N-[(4-bromo-3,5-difluor...

A novel compound crystallizes in the triclinic space group P−1 with a = 7.674(4) Å, b = 12.584(6) Å, c = 15.921(6) Å, α = 89.62(4)°, β = 84.34(4)°, γ = 73.77(4)° and Z = 4. This compound contains Schiff base and rings of molecule has (E) configuration with respect to the central CN double ...

The 2-bromo-N-(4-(7-(diethylamino)-coumarin-3-yl)phenyl)propanamide was synthesized and analyzed by NMR and FT-IR spectroscopies, high resolution mass-spectrometry and single crystal X-ray diffraction. The crystal structure belongs to the monoclinic system, P21/c space group with a = 14.9120(7) ...

BackgroundDrug therapy plays an important role in the treatment of cervical cancer, which is one of the most common solid tumors in women. Therefore, it is important to seek more effective and less toxic therapies.