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.
We have synthesized many metal (II) complexes using curcumin L1 as the major ligand and 2-(1H-Benzimidazol-2-yl) aniline L2 as a supporting ligand. The complexes were characterized by spectroscopy methods such as; molar conductivity, elements microanalysis, Fourier-transform spectroscopy (FT-IR), UV-vis, and mass spectroscopy. Both curcumin ligands and L2 were found to be capable of binding to M(II) and metal ions via their two N atoms, according to the data. The formula for the complexes is the same. [M (L1)(L2)H2OCl], where M is Ni(II), Co(II), Cu(II), Cd(II), and Hg(II) (II). Octahedral complexes are proposed for the prepared compounds. The bio-actives suggested that the complexes are effective against bacteria and fungus on a mi
... Show MoreHistone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc
... Show MoreIn this paper, some chalcone derivatives (C1, C2) were synthesized based on the reaction of equal amount of substituted acetophenone and substituted banzaldehyde in basic medium. Oxazine and thiazine derivatives were prepared from the reaction of chalcones (C1-C2) with urea and thiourea respectively in a basic medium. Pyrazole derivatives were prepared based on the reaction of chalcones with hydrazine mono hydrate or phenyl hydrazine in the presence of glacial acetic acid as a catalyst. The new synthesized compounds were identified using various physical techniques like1 H-NMR and FT-IR spectra.
The present study aimed to synthesize selenium nanoparticles (SeNPs) using aqueous extract of black currant as a reducing agent. The green synthesized black currant selenium nanoparticles (BCSeNPs) were identified by color change. The characterization of SeNPs was achieved by Ultraviolet-visible (UV–VIS) spectroscopy, scanning electron microscopy (SEM), X–ray diffraction analysis (XRD), and Fourier transform infrared spectroscopy (FTIR). These tests were used to detect: stability, morphology, size, crystalline nature, and functional groups present on the surface of BCSeNPs. The results revealed appearance of the brick-red color indicating the specific color of selenium nanoparticles, and UV-Vis spectroscopy showed band absorbanc
... Show MoreA variety of liquid crystals comprising heterocyclics 1,3,4-oxadiazol ring [III], aminooxazol [IV]a, and aminothiazol [IV]b were synthesized through a number of steps, beginning of the reaction of 3, 3'- dimethyl - [1, 1'-biphenyl] -4, 4'- diamin, ethyl monochloroacetate and sodium acetate to synthesize diacetate compound[I]. The diester reacted with hydrazine hydrate(N2H4-H2O) to give dihydrazide compound [II], then reacted with Pyruvic acid and phosphorous oxychloride to produce diketone compound [III]. The last compound was reacted with urea and thiourea to give aminooxazol and aminothiazol respectively. The synthesized compounds actually characterized and determined the structures by melting points, FT-IR and 1H-NMR spectroscopies. By u
... Show MoreComplexes of some metal ions with 2-thiotolylurea were prepared in ethanolic medium using (1:1) (Metal : Ligand) ratio yielded series of neutral complexes as the general formula [M(L)Cl2]. The prepared complexes were identified by atomic absorption FT.IR, UV-Visble spectra, molar conductivity and magnetic properties. From the above data the tetrahedral structure was suggested for all complexes.
Carbon nanospheres (CNSs) were successfully prepared and synthesized by Catalytic Chemical Vapor Deposition (CCVD) by using camphor as carbon source only, over iron Cobalt (Fe-Co) saturated zeolite at temperature between (700 oC and 900 °C), with different concentrations of camphor, and reaction time. The synthesized CNSs were characterized using Scanning Electron Microscopy (SEM), X-ray diffraction spectroscopy (XRD), and Fourier Transform Infrared (FTIR). The carbon spheres in different sizes between 100 nm and 1000 nm were investigated. This work has done by two parts, first preparation of the metallic catalyst and second part formation CNSs by heat treatment.
In our research novel schiff bases of imides moiety have been synthesized . Novel Schiff base derivatives of imides moiety have been synthesized by multistep reaction . First step involves prepare 2-amino -5-mercapto-1,3,4-thiadiazole (I) by the cyclization of thiosemicarbazide with carbon disulphide and anhydrous sodium carbonate in ethanol as a solvent . Then , compound (I) was reacted with phthalic anhydride in the presence of glacial acetic acid to give 2-(5-mercapto-1,3,4-thiadiazol-2-yl) isoindoline-1,3-dion (II).Compound (II)was heated with ethyl chloracetate in the presence of potassium carbonatproduced ethyl 2(5-(1,3-dioxoisoindoline -2-yl)-1,3,4-thiadiazole-2-yl thio) acetate (III).The reaction of compo
... Show MoreBromelain is a proteolytic enzyme rich in cysteine proteases, extracted from the stem and fruit of pineapple (Ananas comosus). There are several therapeutic applications of the bromelain enzyme, where it has anti-inflammatory, anti-cancer, and antimicrobial activity, reduces joint pain, and accelerates wound healing. In the current study, bromelain enzyme was loaded on silver nanoparticles (Br-AgNPs) prepared using the citrate-reduction Turkevich method. Different characterization analyses were performed, including UV-Vis spectrophotometers, FTIR, SEM, and XRD analyses. Moreover, the antioxidant activity of prepared Br-AgNPs was evaluated by DPPH assay. The results of UV-Vis showed a peak at 434 nm, which referred to the AgNPs f
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