The cytotoxic activities of imidazole derivatives prepared from various guanylhydrazone and phenylglyoxal monohydrate

Abstract

A series of imidazole derivatives were synthesized from two-component condensation reaction of phenylgloxal monohydrate with guanylhydrazone. They were characterized by spectroscopic and analytical techniques. The in vitro anticancer evaluation of these compounds was done on human breast cancer (MCF-7) and human liver cancer (HepG2) cell lines using the MTT assay method. Most of the newly synthesized compounds displayed cytotoxic activity against these cancerous cells. In fact, compounds 3a, 3e, and 3?h exhibited more cytotoxic activities than the positive control drugs, fluro-5, and irinocam, against the MCF-7 cell line. Almost all the compounds, except for three, 3b, 3d, and 3f, gave more cytotoxic results than cisplatin. Therefore, these compounds could be considered for further development as anticancer drug candidates.     

Four-Component,One-Pot Synthesis of 2-Aryl-4-Thionylquinoline Derivatives and Their Aromatization

Four-component, one-pot condensation of dimedon, thiophene-2-carbaldehyde, ammonium acetate, and numerous acetophenones yielded novel 2-aryl-4-thionylquinoline derivatives. The structures were characterized by ¹H NMR, ¹³C NMR, IR, and elemental analysis.     

Facile Method for 1,3‐Dipolar Cycloaddition Reaction of Azomethine Ylides: Highly Stereoselective Synthesis of Substituted Pyrrolidine Derivatives

The substituted pyrolidine derivatives with high stereoselectivity were obtained through cycloaddition reaction in the presence of a Lewis acid namely diethylzinc by solvent‐free grinding method.     

Cyclohexenones Through Regioselective Addition of 1,3-Dicarbonyl Compounds to Terpenoid-Like Bischalcones

Terpenoid-like bischalcones (3 and 4) were synthesized from the reaction of α- and β-ionones and benzaldehydes in excellent yields. The Michael addition of 1,3-dicarbonyl compounds to bischalcones (3 and 4) resulted in the formation of cyclohexenones derivatives (10a–d and 14a, b) via regioselective addition of 1,3-dicarbonyls and then cyclization.     

Synthesis and Characterization of New Chalcone Derivatives from cis-Bicyclo[3.2.0]hept-2-en-6-one

A series of chalcone derivatives (3a–k) were prepared via the reaction of cis-bicyclo[3.2.0]hept-2-en-6-one (1) with the respective arylaldehydes (2a–k) and were then characterized by Fourier transform infrared (FT-IR), ¹H NMR, ¹³C NMR, and elemental analyses.     

Alternate Method for the Synthesis of Six-Membered Carbocycles with Five Stereocenters: 1,2,3,4,6-Pentasubstituted-4-hydroxy-cyclohexanes

A series of novel 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes (3a–u) were synthesized from the reaction of aromatic ketones with aromatic aldehydes under mild reaction conditions in good yields. The stereochemistry of the synthesized compounds was established using 1D and 2D-NMR spectra.     

Investigation of radiocesium biokinetics in Manila clam (Ruditapes philippinarum)

This study was carried out to better understand the biokinetics of radiocesium in clams living in sediment. The accumulation and depuration kinetics of ¹³⁴Cs were investigated in the Manila clam (Ruditapes philippinarum) under controlled laboratory conditions. The concentration factor was found to be 3.0 for ¹³⁴Cs in the whole body; however, the concentration factor in the soft part of the clams (12) was significantly higher than those in the whole body and shell (0.80). The depuration kinetics of the radionuclide were described by a two-component exponential model for the whole body. The biological half-lives in the fast and slow components were found to be 0.63 and 22.1 days, respectively. The depuration kinetics for ¹³⁴Cs in the soft parts were described by a single-component exponential model with a resultant the biological half-life of 18.0 days.     

Adsorption of Cd(II) Ions onto Activated Carbon Prepared from Hazelnut Husks

In this study, a batch adsorption of Cd(II) ions onto activated carbon (AC) produced from hazelnut husks were investigated. The factors controlling the adsorption process such as initial pH, agitation time, dosage and initial concentration have been examined. The AC was showed a high affinity to Cd(II) ions at pH values between 5.0 and 7.0. The equilibrium time was found to be 300 minutes. Cd(II) adsorption equilibrium was analyzed with both Langmuir and Freundlich isotherm equations and it was found that Langmuir equations fitted well with the experimental data. Maximum Cd(II) adsorption capacity of AC was calculated to be 20.9 mg g^?1. Cd(II) adsorption kinetics described well with the pseudo second order model. The activated carbon prepared from hazelnut husks is efficient sorbent material for the removal of Cd(II) ions from aqueous solutions.     

Design and Development of Oral Oil-in-Water Nanoemulsion Formulation Bearing Atorvastatin: In Vitro Assessment

The objective of the present investigation was to design a thermodynamically stable and dilutable nanoemulsion formulation of AT-Ca with minimum surfactant concentration that could improve its solubility as well as its oral bioavailability. The composition of optimized nanoemulsion formulation was Sefsol 218 and oleic acid (1:1) 10% w/w, as an oil phase, Tween-20 (19% w/w) as a surfactant, Carbitol (19% w/w) as a cosurfactant and distilled water (52% w/w) as an aqueous phase, containing 10 mg of AT. The optimized formulation showed higher% drug release (99.34%), lower droplet size (42.8 ± 0.42 nm) with low polydispersity index (0.237 ± 0.012), less viscosity (27.51 ± 1.01 cP) and infinite dilution capability. In vitro drug release from the nanoemulsion formulations was highly significant (p < 0.01) as compared to drug suspension.