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.
A new ligand (H4L) and its complexes with ( ZnII, CdII and HgII) were prepared. This ligand was prepared in two steps. In the first step a solution of terephthaldehyde in methanol was reacted under reflux with 1,2-phenylenediamine to give an precursor compound which reacted in the second step with 2,4-dihydroxybenzaldehyde to give the ligand. The complexes were then synthesized by direct reaction of the corresponding metal chloride with the ligand. The ligand and complexes were characterized by spectroscopic methods FT-IR, UV-Vis, 1 HNMR, and atomic absorption, chloride content, HPLC, mole-ratio determination. in addition to conductivity measurement. The data of these measurements suggest a distorted tetrahedral geometry for ZnII, C
... Show MoreA new class of biologically active nanocomposites and modified polymers based on poly (vinyl alcohol) (PVA) with some organic compounds [II, IV, V and VI] were synthesized using silver nanoparticles (Ag-NPs). All compounds were synthesized using nucleophilic substitution interactions and characterized by FTIR, DSC and TGA. The biological activity of the modified polymers was evaluated against: gram (+) (staphylococcus aureus) and gram (-): (Es cherichia coli bacteria). Antimicrobial films are developed based on modified poly (vinyl alcohol) MPVA and Ag-NPs nanoparticles. The nanocomposites and modified polymers showed better antibacterial activities against Escherichia coli (Gram negative) than against Staphyloc
... Show MoreNovel bidentate Schiff bases having nitrogen-sulphur donor sequence was synthesized from condensation of racemate camphor, (R)-camphor and (S)-camphor with Methyl hydrazinecarbodithioate (SMDTC). Its metal complexes were also prepared through the reaction of these ligands with silver and bismuth salts. All complexes were characterized by elemental analyses and various physico-chemical techniques. These Schiff bases behaved as uninegatively charged bidentate ligands and coordinated to the metal ions via ?-nitrogen and thiolate sulphur atoms. The NS Schiff bases formed complexes of general formula, [M(NS)2] or [M(NS)2.H2O] where M is BiIII or AgI, the expected geometry is octahedral for Bi(III) complexes while Ag(I) is expected to oxidized t
... Show Morenew six mixed ligand complexes of some transition metal ions Manganese (II), Cobalt(II), Iron (II), Nickel (II) , and non transition metal ion zinc (II) And Cadmium(II) with L-valine (Val H ) as a primary ligand and Saccharin (HSac) as a secondary ligands have been prepared. All the prepared complexes have been characterized by molar conductance, magnetic susceptibility infrared, electronic spectral, Elemental microanalysis (C.H.N) and AA . The complexes with the formulas [M(Val)2(HSac)2] M= Mn (II) , Fe (II) , Co(II) ,Ni(II), Cu (II),Zn(II) and Cd(II) L- Val H= (C5H11NO2) , C7H5NO3S The study shows that these complexes have octahedral geometry; The metal complexes have been screened for their in microbiological activities against bacteria.
... Show MoreSome new cyclic imides are prepared by the reaction of ampicillin drug with different cyclic anhydrides as a first step to form amic acids for ampicillin drug. The second step includes the reaction of prepared amic acids with acetic anhydride and anhydrous sodium acetate with heating in THF as a solvent to give cyclic imide compounds. These compounds are identified by melting points, FT-IR, 1H-NMR, and biological activity
A new ligand [4-chloro-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3- dihydro-1H-pyrazol-4-ylcarb amothioyl) benzamide] (CAP) was synthesized by reaction of P-ChloroBenzoyl isothio cyanate with 4- aminoantipyrine,The ligand was characterized by micro elemental analysis C.H.N.S.,FT-IR,UV-Vis and1H13CNMR spectra, some transition metals complex of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From the obtained results the molecular formula of all prepared complexes were [M(CAP)2(H2O)2]Cl2(M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg),the proposed geometrical structure for all complexes were octahedral
A new ligand [ 2-chloro-N- (1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro -1H-pyrazol- 4-ylcarbamothioyl)acetamide](L) was synthesized by reacting the Chloro acetyl isothiocyanate with 4-aminoantipyrine,The ligand was characterized by(C HNS) elemental microanalysis and the spectral measurements including Uv-Vis ,IR ,1H and13C NMR spectra, some transition metals complex of this ligand were prepared and characterized by Uv-Vis, FT-IR spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From the obtained results the molecular formula of all prepared complexes were [M(L)2(H2O)2]Cl2 (M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg),the proposed geometrical structure for all complexes were octahedral.
ABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity
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