Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for preliminary detection of products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI possess optimal activity proportional with increased number of 6-MP molecules.
The aim of this paper, study the effect of carbon nanotubes on the electrical properties of polyvinylchloride. Samples of polyvinylchloride carbon nanotubes composite prepared by using hot press technique. The weight percentages of carbon nanotubes are 0,5,10 and 20wt.%. Results showed that the D.C electrical conductivity increases with increasing of the weight percentages of carbon nanotubes. Also, the D.C electrical conductivity changed with increase temperature for different concentrations of carbon nanotubes. The activation energy of D.C electrical conductivity is decreased with increasing of carbon nanotubes concentration.
Nitrogen-comprising heterocyclic compounds and their derivatives have empirically been invaluable as therapeutic agents. Fundamentally, 4-chloro-6-nitro-2-amino-1,3-benzothiazole 1 was synthesized via bromination of 2-chloro-4-nitro aniline with ammonium thiocyanate. This new heterocyclic haloorganoamino-1,3-benzothiazole derivative, was a starting material, which condensed and tethered with three different aromatic aldehyde pendant arm in presence of ethanol and glacial acetic acid isolating an interesting sequence of tridentate Schiff bases 2-4. These compounds were used for complexation reactions in 1:1 (metal: ligand) stoichiometry to obtain heteroleptic Al(III), Ni (II) and K(I) benzothiazole chelat
... Show MoreThe physical and morphological characteristics of porous silicon (PS) synthesized via gas sensor was assessed by electrochemical etching for a Si wafer in diluted HF acid in water (1:4) at different etching times and different currents. The morphology for PS wafers by AFM show that the average pore diameter varies from 48.63 to 72.54 nm with increasing etching time from 5 to 15min and from 72.54 to 51.37nm with increasing current from 10 to 30 mA. From the study, it was found that the gas sensitivity of In2O3: CdO semiconductor, against NO2 gas, directly correlated to the nanoparticles size, and its sensitivity increases with increasing operating temperature.
Objectives: Two derivatives of cephalexin were synthesized by reaction with isatin-glycine Schiff base and bromoisatin-glycine Schiff base separately. Methods: Cephalexin was linked through the amine group to isatin glycine and bromoisatin glycine Schiff bases by amide bond formation. Results: These derivatives were characterized by FT-IR, H-NMR, elemental CHN analysis and then tested for their antimicrobial activity compared to cephalexin against gram-positive, gram-negative bacteria and Candida albicans fungi. Conclusion: The two compounds showed better activity against Staphylococcus aureus, compound 3b is more active against Escherichia coli, and compound 3a is more active against Klebsiella pneumonia.
This research discloses the synthesis of various polyester resins, the polyesters containing homoring aromatic and others heterocyclic were synthesized by the condensation polymerization of suitable monomers (which are containing variety function groups in different structures) with phthalic anhydride. The main objective is synthesis of new polyester with keeping a reasonable electrical insulating behavior. The structural of polymer was characterized by Fourier Transform infra-red spectroscopy FTIR and HNMR. The dielectric constant (real ε' and imaginary parts ε") and AC conductivity (σAC) for all the polyester samples are studied by varying the frequency (30, 50, 70, 90, 120, 300, 500Hz and 1KHZ) at 25⁰ C. Indeed, study of the electri
... Show MoreA new two series of liquid crystalline Schiff bases containing thiazole moiety with different length of alkoxy spacer were synthesized, and the relation between the spacer length and the liquid crystalline behavior was investigated. The molecular structures of these compounds were performed by elemental analysis and FTIR, 1HNMR spectroscopy. The liquid crystalline properties were examined by hot stage optical polarizing microscopy (OPM) and differential scanning calorimetry (DSC). All compouns of the two series display liquid crystalline nematic mesophase. The liquid crystalline behaviour has been analyzed in terms of structural property relationship
The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1
... Show MoreIn the present study, ( Schiff's bases 6a - 6e) and (new amids derivatives 6f - 6j) have been synthesized . The glutaroyl chloride(2) has been prepared by the reacting of glutaric acid and thionyl chloride in presence of (DMF) . The new compound bis(4-formylphenyl) glutarate (3) has been Synthesized from reaction of one mole of glutaroyl chloride and two moles of 4-hydroxybenzaldehyde . Compound 4,4'-(glutaroylbis(oxy))dibenzoic acid (4) was Synthesized from one mole of glutaroyl chloride and two moles of 4-hydroxybenzoic acid, while compound bis(4-(chlorocarbonyl)phenyl) glutarate (5) was prepared from 4,4'-(glutaroylbis(oxy))dibenzoic acid and Thionyl chloride . Then Schiff's bases 6a - 6e that prepared
... 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. (
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