The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis of the target compounds was accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug selectively into the cancer cells to be hydrolyzed by enzymes that are elevated in tumor tissues compared with normal tissues . Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.
D-mannose sugar was used to prepare [benzoic acid 6-formyl-2, 2-dimethyl-tetrahydrofuro [3, 4-d][1, 3] dioxol-4-yl ester](compound A). The condensation reaction of folic acid with (compound A) resulted in the formation of new ligand [L]. These compounds were characterized by elemental analysis CHN, atomic absorption AA,(FT-IR),(UV-Vis), TLC, ES mass (for electrospray), molar conductance, and melting point. The new tetradentate ligand [L], reacted with two moles of some selected metal ions and two moles of (2-aminophenol),(metal: ligand: 2-aminophenol) at reflux in water medium to give a series of new complexes of the general formula K2 [M2 (L)(HA) 2] where M= Co (II), Ni (II), Cu (II) and Cd (II). These complexes were characterized by eleme
... Show MoreD-mannose sugar was used to prepare [benzoic acid 6-formyl-2,2-dimethyl-tetrahydrofuro[3,4-d][1,3]dioxol-4-yl ester] (compound A). The condensation reaction of folic acid with (compound A) resulted in the formation of new ligand [L]. These compounds were characterized by elemental analysis CHN, atomic absorption A.A, (FT-I.R.), (U.V.-Vis), TLC, E.S. mass (for electrospray), molar conductance, and melting point. The new tetradentate ligand [L], reacted with two moles of some selected metal ions and two moles of (2-aminophenol), (metal : ligand : 2-aminophenol) at reflux in water medium to give a series of new complexes of the general formula K2[M2(L)(HA)2] where M= Co(II), Ni(II), Cu(II) an
... Show MorePrevious studies on the synthesis and characterization of metal chelates with uracil by elemental analysis, conductivity, IR, UV-Vis, NMR spectroscopy, and thermal analysis were covered in this review article. Reviewing these studies, we found that uracil can be coordinated through the electron pair on the N1, N3, O2, or O4 atoms. If the uracil was a mono-dentate ligand, it will be coordinated by one of the following atoms: N1, N3 or O2. But if the uracil was bi-dentate ligand, it will be coordinated by atoms N1 and O2, N3 and O2 or N3 and O4. However, when uracil forms complexes in the form of polymers, coordination occurs through the following atoms: N1 and N3 or N1 and O4.
The aim of the work is synthesis and characterization of bidentate ligand [3-(3-acetylphenylamino)-5,5-dimethylcyclohex-3-enone][HL], from the reaction of dimedone with 3-amino acetophenone to produce the ligand [HL], the reaction was carried out in dry benzene as a solvent under reflux. The prepared ligand [HL] was characterized by FT-IR, UV-Vis spectroscopy, 1H, 13C-NMR spectra, Mass spectra, (C.H.N) and melting point. The mixed ligand complexes were prepared from ligand [HL] was used as a primary ligand while 8-hydroxy quinoline [HQ] was used as a secondary ligand with metal ion M(Π).Where M(Π) = (Mn ,Co ,Ni ,Cu ,Zn ,Cd and Pd) at reflux ,using ethanol as a solvent, KOH as a base. Complexes of the composition [M(L)(Q)] with (1
... Show MoreThis work includes preparation of Az, Qz, and Tz derivatives from the reaction of Schiff base (Sb) derivative with anthranilic acid, chloroacetyl chloride, and sodium azide, as well as, the characterization via FT-IR, 1H-NMR, and 13CNMR. The anticorrosion inhibition of these compounds was studied and the measurements of carbon steel (CS) corrosion in sodium chloride solution 3.5% (blank) and inhibitor in solutions were calculated at a temperature range of 293-323 K by the technique of electrochemical polarization. In addition, some thermodynamic and kinetic activation parameters for inhibitor and blank solutions (Ea⋇, ΔH⋇, ΔS⋇, and ΔG⋇) were determined. The results showed high inhibition efficacy for all the prepared compounds,
... Show MoreThe newly synthesized Schiff base ligand (E)-2-((2-phenylhydrazono)methyl)naphthalen-1-ol (phenyl hydrazine derivative), is allowed to react with each of the next mineral ion: Ni2+, Cu2+, Zn2+andCd2+successfully resulting to obtain new metal complexes with different geometric shape. The formation of Schiff base complexes and also the origin Schiff base is indicated using LC-Mass that manifest the obtained molar mass, FT-IR proved the occurrence of coordination through N of azobenzene and O of OH by observing the shifting in azomethines band and appearing of M-N and N-O bands. Moreover, we can also detect by such apparatus, the presence of aquatic water molecule inside the coordination sphere. UV-Vis spectra of all resultants reveale
... Show MoreA variety of new phenolic Schiff bases derivatives have been synthesized starting from Terephthaladehyde compound, all proposed structures were supported by FTIR, 1H-NMR, 13C-NMR, Elemental analysis, some derivatives evaluated by Thermal analysis (TGA).
A new two series of liquid crystalline Schiff bases containing thiazole moiety with different length of alkoxy spacer were synthesized, and the relation between the spacer length and the liquid crystalline behavior was investigated. The molecular structures of these compounds were performed by elemental analysis and FTIR, 1HNMR spectroscopy. The liquid crystalline properties were examined by hot stage optical polarizing microscopy (OPM) and differential scanning calorimetry (DSC). All compouns of the two series display liquid crystalline nematic mesophase. The liquid crystalline behaviour has been analyzed in terms of structural property relationship
Coblatcomplex has been prepared by reaction between C16H19N3O3S (L) as ligand and metal salt (II). The prepared complex were characterized by infrared spectra, electromic spectra, magnetic susceptibility, molar conductivity measurement and metal analysis by atomic absorption and (C.H.N) analysis. From these studies tetrahedral geometry structure for the complex was suggested. The photodegredation of complex were study using photoreaction cell and preparednanoTiO2 catalyst in different conditions (concentration, temperatures, pH).The results show that the recation is of a first order with activation energy equal to (6.6512 kJ /mol).
The synthesis, characterization and liquid crystalline properties of N4,N40 -bis((1 H-benzo[d]imidazol-2- yl)methyl)-3,30 -dimethyl-[1,10 -biphenyl]-4,40 -diamine and of their corresponding Mn(II), Fe(II), Ni (II), Cu(II), and Zn(II) complexes are described. The ligand and complexes have been characterized by elemental analysis, magnetic susceptibility measurements (meff), conductometric measurements and Fourier Transform Infrared (FTIR), Nuclear Magnetic Resonance (1 H NMR), (13C-NMR) and UV–Vis spectroscopy. Spectral investigations suggested octahedral coordination geometrical arrangement for M(II) complexes. The phase transition temperatures were detected by differential scanning calorimetry (DSC) analysis and the phases are confirmed
... Show More