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.
الوصف The synthesis of 2 (N-phenyl dithio carboxamid) benzothiazol Ligand (L) from reaction of 2-Mercaptobenzothiozol with phenylisothiocyanate using ratio 1: 1. The ligand was characterized by elemental analysis (CHN),'H-NMR, IR and UV-Vis. The complexes with bivalent ions (Ni, Cu, Zn, Cd and Hg) have been prepared and characterized. The structural diagnosis was established using IR, UV–Visible spectro photometer, molar conductivity, atomic absorption and molar ratio with selected metal ions (Ni2+, Cu2+). The complexes of (Ni, Cu) gave octahedral structural while the complexes of (Zn, Cd, Hg) gave tetrahedral structural. The study of biological activity of the ligand (L) and its complexes (Ni, Cu, Hg) in two deferent concentration (
... Show MoreThe aim of this research is to employ starch as a stabilizing and reducing agent in the production of CdS nanoparticles with less environmental risk, easy scaling, stability, economical feasibility, and suitability for large-scale production. Nanoparticles of CdS have been successfully produced by employing starch as a reducing agent in a simple green synthesis technique and then doped with Sn in certain proportions (1%, 2%, 3%, 4%, and 5%).According to the XRD data, the samples were crystallized in a hexagonal pattern, because the average crystal size of pure CdS is 5.6nm and fluctuates in response to the changes in doping concentration 1, 2, 3, 4, 5 %wt Sn, to become 4.8, 3.9, 11.5, 13.1, 9.3 nm respectively. An increase in crystal
... Show MoreThis work has been done to prepare a series of new alkene compounds derived from 4-thiozolidinones by substituting different aldehydes, P-acetamido-phenol, and 2-mercapto-benzoimidazole, which were used as starting materials to form ester [I]a,b and then make hydrazides [II]a,b, which were used to prepare 1, 3, and 4-oxadiazoles [III]a,b, which were then used for prepared Schiff bases [IV]a-f, The next step was the synthesis of 4-thiazoldinone derivatives [V]a-f from Schiff bases. The final step was the synthesis of alkenes [VII]a-f, the prepared derivatives were identified with spectral methods (FT-IR, 1H-NMR, mass, and CHNS). The antibacterial activity of the prepared derivatives was evaluated against four types of bacteria, pos
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CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl.
5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM an
... Show MoreIn the present study, the effect of Zinc nanoparticles on levels of (T3 , T4 and TSH) hormones was investigated. Zinc nanoparticles were synthesized by Laser induced plasma.The Nd: YAG Nd: YAG laser with a wavelength of 1064 nm was used to generate nanomaterials of the elements (zinc) upon collision with target atoms. Plasma generated by different laser intensity is generated. After confirming the preparation of zinc nanoparticles, XRD, AFM was examined, and the effect of these substances on the thyroid gland (T3, T4, TSH) was observed for two doses of each component (1 ml / kg, 4 ml / kg) after conducting a cytotoxicity examination of the lymphocytes of the rats extracted from Rat spleen was 1.8% less toxic to zinc, and as noted The
... Show MoreThis research include synthesized and characterization the compound [I] by reaction terephthaldehyde , mercaptoacetic acid and thiosemicarbazide with concentrated sulfuric acid then this compound reaction with ethyl chloroacetate and sodium acetate to product ester compound [II],the latter compound reaction with hydrazine hydrate to synthesized acid hydrazide [III] after that reaction with 4-alkoxy benzaldehyde[IV]n to synthesized Schiff bases compounds [V]n, the compound [VI] synthesized via reaction compound [I] with chloroacetic acid and sodium acetate then the compound[VI] reaction with 2-phenylenediamine in 4 N hydrochloric acid to product benzimidazole compound[VII]. The compounds characterized by melting points, FTIR and 1HNMR spectr
... Show MoreSilica-based mesoporous materials are a class of porous materials with unique characteristics such as ordered pore structure, large surface area, and large pore volume. This review covers the different types of porous material (zeolite and mesoporous) and the physical properties of mesoporous materials that make them valuable in industry. Mesoporous materials can be divided into two groups: silica-based mesoporous materials and non-silica-based mesoporous materials. The most well-known family of silica-based mesoporous materials is the Mesoporous Molecular Sieves family, which attracts attention because of its beneficial properties. The family includes three members that are differentiated based on their pore arrangement. In this review,
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