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bijps-381
Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
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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.

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Publication Date
Fri May 02 2014
Journal Name
International Journal Of Scientific & Technology Research
Synthesis, Structure And Characterization Of Zns Qds And Using It In Photocatalytic Reaction
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ZnS nanoparticles were prepared by a simple microwave irradiation method under mild condition. The starting materials for the synthesis of ZnS quantum dots were zinc acetate (R & M Chemical) as zinc source, thioacetamide as a sulfur source and ethylene glycol as a solvent. All chemicals were analytical grade products and used without further purification. The quantum dots of ZnS with cubic structure were characterized by X-ray powder diffraction (XRD), the morphology of the film is seen by scanning electron microscopy (SEM). The particle size is determined by field effect scanning electron microscopy (FESEM), UV-Visible absorption spectroscopy and XRD. UV-Visible absorption spectroscopy analysis shows that the absorption peak of the as-prep

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Publication Date
Wed Oct 13 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis and Characterization and Thermal Properties of New Linked Azo-Phenol-Formaldehyde Resins
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Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of Schiff Base Folic Acid Based Ligand and Its Complexes
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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

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Publication Date
Fri Apr 01 2005
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of Schiff Base Folic Acid Based Ligand and Its Complexes
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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 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) and Cd(II). These complexes were characterized by elem

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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Physics: Conference Series
Mixed Ligand Complexes of Schiff Base and Nicotinamide: Synthesis, Characterization and Antimicrobial Activities
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A new Schiff base of HL has been synthesized from amoxicillin drug and 4- Chlorobenzophenone. Cr (III), Fe (III), Co (II), Ni (II), Cu (II), Cd (II) and Hg (II) mixed ligands complexes of Schiff base and Nicotinamide. Diagnosis of synthesis ligand and its complexes are done by 1HNMR, 13CNMR and thermal analysis for HL ligand, FTIR, UV-visible, molar conductance, CHN analysis, magnetic susceptility and atomic absorption. Octahedral geometries have been suggested for all complexes. All compounds under study were tested antimicrobial activity against four type of bacteria such as Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus Bacillis subtilis in nutrient agar.

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Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis and Characterization of some Tetrazole Derivatives and Evaluation of their Biological Activity
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Publication Date
Sat Apr 01 2023
Journal Name
Russian Journal Of General Chemistry
Synthesis and Characterization of Metals Complexes with Uracil and Uracil Derivatives (A Review)
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Publication Date
Sat Nov 04 2023
Journal Name
Russian Journal Of General Chemistry
Synthesis and Characterization of Metals Complexes with Uracil and Uracil Derivatives (A Review)
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Previous 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.

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Publication Date
Sat Dec 01 2018
Journal Name
Indian Journal Of Natural Sciences
Leishmanicidal Activity of Methotrexate against Leishmania tropica Promastigotes
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Leishmaniasis is one of the neglected parasitic diseases, which belongs to the family Trypanosomatidae. Cutaneous leishmaniasis is endemic in Iraq and the available drugs are of side effect or resistant by the parasite. In this study, cytotoxicity of methotrexate was investigated on the promastigotes proliferation of the Iraqi strain ofL.tropica.The results showed a significant (p ≥ 0.05) difference in growth of treated groupsat all concentration (1000, 500, 250, 125.5, 62.5, 31.25, 15.6) μM, after 24 and 48 hours of follow up, while after 72 hours, significant difference was observed at concentration(1000, 125, 62.5) μM.The IC50 measured after 24and 48 hours and it was 40.366 and 44.452 μM, respectively.The present study showed

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Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Pharmacy And Biological Sciences
Cytotoxic Effect of Methotrexate on Leishmania donovani Promastigotes
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Leishmania is auxotroph to folic acid,antifolates drug inhibit the synthesis and conversion of folate derivatives. In this study, cytotoxic effect of methotrexate was investigated on the procyclic promastigotes proliferation of L. donovani. The results showed a significant (p ≥ 0.05) difference in growth of treated groups at high concentrations (1000, 500, 250, 125.5) μM after 24, 48 hrs., while at 72 hrs. significant difference was observed at all concentration. The IC50 values was measurable after 24, 48 and 72 hrs. and it was 174.238, 52.283 and 109.175 μM, respectively. The present study showed the cytotoxic effect of methotrexate on the proliferation of promastigotes of the visceral type of Leishmania.

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