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.
6-(2-benzathiazolyl azo),-3,5-dimethylphenol was formed by grouping the 2- benzothiazole diazonium chloride with 3,5-dimethylphenol. Azo ligand(L) was resolved on the origin by 1H and 13CNMR, FTIR and UV-V is spectral analysis. Complexation of tridentate ligand (L) with Co2+, Ni2+, Cu2+ and Zn2+ in aqueous of ethyl alcohol with a 1:2 metal:ligand, and at ideal pH.. The formation of metal chelates are assigned using flame atomic, absorption, FTIR, and UV-Vis spectral analysis, other than conductivity and magnetic estates. The nature of the metal chelates were carried out by mole ratio and continuous, variation mechanism, Beer's law, followed the rate (0.0001 - 3×0.0001 M) concentration., High molar, absorptivity, for the complex solutions w
... Show MoreThin films were prepared from poly Berrol way Ketrrukemaaih pole of platinum concentrations both Albaarol and salt in the electrolytic Alastontrel using positive effort of 7 volts on the pole and the electrical wiring of the membrane record
In this research some new nucleoside analogues were synthesized. Starting from α-D- glucose which was protected to glucose penta acetat α-D- glucose pyronside (1). Which was converted to active form 1-bromo protected sugar (2) as a sugar moiety. The base moiety 2-substituted imidazoline (3,4) was prepared from condensation of ethylene diamine with two kind of aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleaobase derivatives (5-10). Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues (11-16). De blocking of these nucleoside analogues with sodium methoxide in methanol afforded our targe
... Show MoreThe synthesis of gold nanoparticles AuNPs was achievedby the reduction of sodium tetrachloroaurate (III) (NaAuCl4) with ceftriaxone sodium (CR) in aqueous solutionswithout the use of other reducing agent. The effect of reactants concentration, temperature and pH on the sizes and morphology of AuNPs were also studied. The synthesized AuNPs were characterized by UV- visible spectroscopy, X-ray diffraction (XRD), scanning electron microscope (SEM), and atomic force microscope (AFM) analysis. Conjugation of antibiotic with the nanoparticles was characterized by FTIR spectrophotometry.
Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c
... Show More4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoic acid was synthesized from multisteps and converted to their corresponding hydrazide. The corresponding hydrazide was cyclized to their corresponding 5-amino-1,3,4-oxadizole. Newly Schiff bases (7a-7e) were synthesized from reaction the 5-amino-1,3,4-oxadizole with several substituted of 4-hydroxybenzylaldehyde. The resulting compounds were characterized based on their IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the synthesized compounds. Compound 7d and 7e exhibited significant free-radical scavenging ability in both assays.
In this work, the study of
Ortho amino hydrazobenzene (L) has been prepared from the reaction of ortho amino phenyl thiol with phenyl hyrazan in mole ratio(1:1). It has been characterized by elemental analysis (C, H, N), IR, UV–Vis. The complexes of the bivalent ions (Co, Ni, Cu, Zn, Pd, Cd, Hg and Pb) and the trivalent (Cr) have been prepared and characterized too. The structural have been established by elemental analysis(C,H,N), IR , UV – Vis spectra , conductivity measurements , atomic absorption and magnetic susceptibility . The complexes showed characteristic behaviour of octahedral geometry around the metal ion and the( N,N) ligand coordinated in bidentate modeexcept with pd showed square planer. ? ,kf , ?max for the complexes were estimated too . ? for Co
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