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 azo dye (LH) was used to synthesize a series of complexes with Fe(III), Co(II), Ru(III), and Rh(III) metal ions. The ligand (LH) was synthesized by the condensation reaction between tryptamine and 2-hydroxyquinoline. Due to the presence of effective donor atoms (-N=N- azo and OH hydroxyl groups), the ligand was subsequently refluxed with various metal ions, leading to the formation of nonelectrolytic [M:L] (1:2). These compounds were characterized using 1H and 13C-NMR, FT-IR, UV–Vis, mass spectrometry, TGA, DSC, and C.H.N. analysis, along with conductivity, magnetic susceptibility, and metal and chlorine content measurements. The results indicated that the ligand acts as a bidentate, with the complexes adopting an octahedral geometry.
... Show MoreTo synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show MoreThe presence of a single complex adaptive weight in each element channel of an adaptive array antenna is sufficient for processing of narrowband signals. The ability of an adaptive array antenna to null interference deteriorates rapidly as the interference bandwidth increases. The performance of narrowband adaptive array antenna with LMCV Beamforming algorithm is examined. The interaction effects between received signal angle of arrival and array parameters like the interelement spacing and the number of array element and the received signal bandwidth were studied. The output Signal to Interference plus Noise Ratio (SINR) and Interference to Noise Ratio (INR) are used as performance parameters for evaluation of these effects. It is found
... Show MoreAzo ligand 11-(4-methoxyphenyl azo)-6-oxo-5,6-dihydro-benzo[4,5] imidazo[1,2-c] quinazoline-9-carboixylic acid was derived from 4-methoxyaniline and 6-oxo-5,6-dihydro-benzo[4,5]imidazo[1,2-c]quinazoline-9-carboxylic acid. The presence of azo dye was identified by elemental analysis and spectroscopic methods (FT-IR and UV-Vis). The compounds formed have been identified by using atomic absorption in flame, FT.IR, UV-Vis spectrometry magnetic susceptibility and conductivity. In order to evaluate the antibacterial efficiency of ligand and its complexes used in this study three species of bacteria were also examined. Ligand and its complexes showed good bacterial efficiencies. From the obtained data, an octahedral geometry was proposed for all p
... 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
... Show MoreAllosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.
A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR
Amoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
This study involved preparation of Graphene oxide (GO) and reduced graphene oxide (RGO) using Hummer method and chemical method respectively. These carbon nanomaterials were used as starting material to make novel functionalize with thiocarbohydrazide (TCH) which was prepared by reacting CS2 with hydrazine to form GO or RGO- 4-amino,5-substituted 1H,1,2,4 Triazole 5(4H) thion (ASTT) ,(GOT) and( RGOT) respectively via cyclocondensation reaction. Also MnO2 nanorod was prepared to form hybridized with GOT and RGOT. A commercial multiwall carbon nanotube (MWCNT) and functionalization with carboxylic groups' (f-MWCNT) and its nanocomposite with GOT were also prepared. All carbon nanomaterials were characterized with different techniques such as
... Show MoreThis study aimed to fabricate a curcumin@platinum nanohybrid (CUR@Pt NPs) through a green tea–based synthesis method and to evaluate its various functions, including antioxidant, burn-healing, and selective anticancer activities against PANC-1 pancreatic cancer cells. Green tea polyphenols served as natural reducing and stabilizing agents, facilitating an eco-friendly, single-step manufacturing process. Physicochemical characterization confirmed successful nanohybrid formation: a CUR@Pt band appeared at 457 nm in the UV–Vis spectrum, XRD displayed crystalline platinum peaks at 2θ = 46.9°, and 67.0°, matching the (200), and (220) planes, respectively, and TEM images showed well-dispersed spherical nanoparticles with an average siz
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