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 work a Nd:YVO4 thin disc laser setup is designed and fabricated. The disk laser system
is designed to be compact. The laser crystal was pumped by a 808 nm diode laser. The effect of input
current and pulse frequency on the output energy at pulse operation mode, and the effect of the input
current on the output power at CW mode operation are tested. At the pulsed mode, the output energy
increased linearly with the input current and decreased with pulse frequency. The threshold current
increased with increasing pulse frequency increasing. The maximum output energy from the thin disc
laser was 0.98 μJ at 1.3 kHz frequency, with 0.49A. A minimum threshold current for CW mode of
operation. The maximum outpu
Background: Maxillary first premolar with wide MOD cavity more susceptible to fracture. The aim of this study was to assess the influence of cavity design for cusp coverage on the fracture resistance of weakened maxillary first premolar restored with CAD/CAM hybrid ceramic versus nanohybide composite. Materials and Methods: Fifty six intact maxillary first premolars of approximately comparable sizes were divided into seven groups eight for each: Group A: Intact teeth (control group); Group B: teeth prepared for MOD inlay; Group C: teeth prepared for MOD onlay covering the lingual cusp; Group D: teeth prepared for MOD covering buccal and lingual cusps ,the previous three groups indirectly restored with nanohybrid composite (3M ESPE Z 250 X
... Show MoreIn this work, prepared new ligand[3- (1H-indol-3-yl) -2- (3-(4- methoxybenzoyl)thiouereido) propanoic acid](MTP) has been synthesized by reaction of 4-Methoxybenzoyl isothiocyanate with tryptophane(1:1), The ligand was characterized by elemental microanalysis C.H.N.S, FT-IR, UV-Vis and 1H,13C NMR spectra, Some transition metals complexes of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption, From obtained results the molecular formula of all prepared complexes were [M(MTP)2] (M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg), the proposed geometrical structure for all complexes were tetrahedral except copper complex has a square planer geometry around metallic ion
... Show MoreA series of metal ion complexes of some divalent transition metal ions having the general composition [ML2Cl2]nH2O with 2-(benzo[d]thiazol-2-ylamino)-2- (5-chloro-2-hydroxy phenyl) acetonitrile ligand has been prepared from 5-chloro-2-hydroxy-benzaldehyde and benzo[d]thiazol-2-amine. Existence of cyanide as potassium cyanide in acidic medium was considered, characterized by elemental chemical analysis, conductance of molarity, magnetic susceptibility measurements, FTIR electronic spectral studies and mole ratio method. FTIR indicates the participation of amino and acetonitrile nitrogen which is coordinated with the central metal ion.
In this research, the preparation of bidentate Schiff base was carried out via the condensation reaction of both the salicylaldehyde with 1-phenyl-2,3-dimethyl-4-amino-5-oxo-pyrazole to form the ligand (L). The mentioned ligand was used to prepare complexes with transition metal ions Mn(II), Co(II), Ni(II), Cu(II) and Zn(II). The resulting complexes were separated and characterized by FTIR and UV-Vis spectroscopic technique. Elemental analysis for Carbon, Hydrogen and Nitrogen elements, electronic spectra of the ligand and complexes were obtained, and the magnetic susceptibility tests were also achieved to measure the dipole moments. The molar conductivities were also measured and determination of chlorine content in the complexes and
... Show MoreBackground: Although mammography is a powerful screening tool in detection of early breast cancer, it is imperfect, particularly for women with dense breast, which have a higher risk to develop cancer and decrease the sensitivity of mammogram, Automated breast ultrasound is a recently introduced ultrasonography technique, developed with the purpose to standardize breast ultrasonography and overcome some limitations of handheld ultrasound, this study aims to evaluate the diagnostic efficacy of Automated breast ultrasound and compare it with handheld ultrasound in the detection and characterization of breast lesions in women with dense breasts. Objectives: To evaluate the diagnostic efficacy of Automated breast ultrasound and compare
... Show MoreBackground: Although mammography is a powerful screening tool in detection of early breast cancer, it is imperfect, particularly for women with dense breast, which have a higher risk to develop cancer and decrease the sensitivity of mammogram, Automated breast ultrasound is a recently introduced ultrasonography technique, developed with the purpose to standardize breast ultrasonography and overcome some limitations of handheld ultrasound, this study aims to evaluate the diagnostic efficacy of Automated breast ultrasound and compare it with handheld ultrasound in the detection and characterization of breast lesions in women with dense breasts.
Objectives:<
... Show MoreThe reaction of 2-amino-benzothiazole with bis [O,O-2,3,O,O – 5,6 – (chloro(carboxylic) methiylidene) ] – L – ascorbic acid (L-AsCl2) gave new product 3-(Benzo[d]Thaizole-2-Yl) – 9-Oxo-6,7,7a,9-Tertrahydro-2H-2,10:4,7-Diepoxyfuro [3,2-f][1,5,3] Dioxazonine – 2,4 (3H) – Dicarboxylic Acid, Hydro-chloride (L-as-am)), which has been insulated and identified by (C, H, N) elemental microanalysis (Ft-IR),(U.v–vis), mass spectroscopy and H-NMR techniques. The (L-as am) ligand complexes were obtained by the reaction of (L-as-am) with [M(II) = Co,Ni,Cu, and Zn] metal ions. The synthesized complexes are characterized by Uv–Visible (Ft –IR), mass spectroscopy molar ratio, molar conductivity, and Magnetic susceptibility techniques. (
... Show MoreNewly 4-amino-1,2,4-triazole-3-thione ring 2 was formed at position six of 2-methylphenol from the reaction of 6-(5-thio1,3,4-oxadiazol-2-yl)-2-methylphenol 1 with hydrazine hydrochloride in the presence of anhydrase sodium acetate. Seven newly fused heterocyclic compounds were synthesized from compound 2. First fused heterocyclic was 6-(6-(3,5-di-tertbutyl-4-hydroxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl)-2-methylphenol 3 synthesized from reaction compound 2 with 3,5-di-tert-butyl-4-hydroxybenzoic acid in POCl3. Reaction compound 2 with bromophencylbromide afford 6-(6-(4-bromophenyl)-5H-[1,2,4]triazolo[3,4-b][1,3,4]-thiadiazin-3-yl)-2-methylphenol 4. 6-(6-thio-1,7a-dihydro-[1,2,4] triazolo[3,4-b][1,3,4]-thiadiazol-3-yl)-2
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