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.
In this present work, [4,4`-(biphenyl-4,4`-diylbis(azan-1-yl-1-ylidene))bis(methan-1-yl-1-ylidene)bis(2-methoxyphenl)(A1),4,4`-(biphenyl-4,4`-diylbis(azan-1-yl-1-ylidene))bis(methan-1-yl-1-ylidene)diphenol(A2),1,1`-(biphenyl-4,4`-diylbis(azan-1-yl-1-ylidene))bis(methan-1-yl-1-ylidene) dinaphthalen-2-ol (A3)]C.S was prepared in 3.5% NaCl. Corrosion prevention at (293-323) K has been studied by using electrochemical measurements. It shows that the utilized inhibitors are of mixed type based on the polarization curves. The results indicated that the inhibition efficiency changes were used with a change according to the functional groups on the benzene ring and through the electrochemical technique. Temperature increases with corrosion current
... Show MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
... Show MoreIn this study, chalcones were synthesis by condensing 2-acetylpyridine with aromatic aldehyde derivatives in dilute ethanolic potassium hydroxide solution at room temperature according to Claisen-Schmidt condensation. After that, new heterocyclic derivatives such as Oxazine, Thiazine and Pyrazol were synthesis by reaction between chalcones with urea, thiourea and hydrazine hydrate respectively scheme 1. All these compounds wrer characterization by FTIR, 1H-NMR spectroscopy and elemental analysis.
The MTX was converted to MTX nanoparticles by the modified method based on changing the pH gradually . For the first time MTX NPs+Meropenem complex were prepared and evaluated as a potential tool to overcome antimicrobial resistance and to improve pharmacokinetics of the drug, the results showed that the antibacterial activity of complex (MTX NPs plus MEM) has increased (from 1( µg/ml) to >0.5( µg/ml) for p1 , from 2( µg/ml) to 1( µg/ml) for p10 and from 8( µg/ml) to 4( µg/ml) for p48).
In this review, previous studies on the synthesis and characterization of the metal Complexes with paracetamol by elemental analysis, thermal analysis, (IR, NMR and UV-Vis (spectroscopy and conductivity. In reviewing these studies, the authors found that paracetamol can be coordinated through the pair of electrons on the hydroxyl O-atom, carbonyl O-atom, and N-atom of the amide group. If the paracetamol was a monodentate ligand, it will be coordinated by one of the following atoms O-hydroxyl, O-carbonyl or N-amide. But if the paracetamol was bidentate, it is coordinated by atoms (O-carbonyl and N-amide), (O-hydroxyl and N-amide) or (O-carbonyl and O-hydroxyl). The authors also found that free paracetamol and its complexes have antimicrobial
... Show MoreA new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag
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