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.
Background: Denture relining is the process of resurfacing of the tissue side of the ill fitting denture, the bond strength at the relining-denture base interface is most important for denture durability.The aim of present study was to evaluate the shear bond strength between the thermosens as relining material and different denture base materials that bonded by thermo fusing liquid. As this corrective procedureis the common chair side procedure in the dental clinic. Material and method: Sixty samples were prepared and divided into three main groups according to the type of denture base materials.Group (A) referred to the heat cure acrylic samples which consisted of 20 samples. Group (B) referred to the high impact acrylic samples which con
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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 MoreSynthesis, Characterization And Biological Evaluation of New Schiff Bases MixedLigand Metal Complexes of Some Drug Substances
This research includes synthesis of new heterocyclic derivatives of N-benzyl-5-bromoisatin. New 1, 2, 4-triazole, oxazoline and thiazoline derivatives of [N-benzyl-5-bromo-3-(Ethyliminoacetate)-indole-2-one] (2) have been synthesized. The preparation process started by the reaction of 5-bromoisatin with sodium hydride in dimethylformamide (DMF) at 0°C, gave suspension of sodium salt of 5-bromoisatin and subsequent reaction with benzylchloride to give N-benzyl-5-bromoisatin (1). Compound (1) reacted with ethylglycinate (Schiff base) obtained the intermediate compound (2) which reacted with different reagents in two ways. The first way, compound (2) reacted with (hydrazine hydrate, semicarbazide, phenylsemicarbazide and thiosemicarbazide)
... Show MoreNew schiff bases series (VIII) a-e and 1,3-thiazolidin-4-one derivatives (IX) a-e containing the 1,2,4-triazole and 1,3,4-thiazazole rings were synthesized and screening their biological activities. These compounds were identified via Fourier transform infrared (FT-IR) spectra, some via Proton nuclear magnetic resonance (1H-NMR) and mass spectra. The biological results indicated that all of these compounds did not reveal antibacterial effectiveness against (Escherichia coli and Klebsiella species) (G-). Some of these compounds showed moderate antibacterial activity against (Staphylococcus aureus, and Staphylococcus epidermidis) (G+), and all compounds exhibited moderate activity against Candida albicans.
This study outlines the synthesis of substituted 1,2,4-triazole derivatives through the cyclization reaction of thiourea derivatives. The process begins with the reaction of different halides with KSCN to produce isothiocyanate derivatives. then followed by a reaction with isonicotinic acid hydrazide to yield thioureas (1-6), with a yield rate of (72-88%). Then, compounds (1-6) were treated with alkaline medium 4 N (NaOH) to produced 1,2,4-triazole derivatives (7-12) with a yield (51-69%).The structure of the prepared compounds was characterized using FTIR,1HNMR and 13CNMR spectroscopy. Some of the synthesized compounds were tested for antimicrobial activity when, compound 9 showed strong activity against gram positive bacteria (Sta
... Show MoreSurvivin, a member of inhibitor of apoptosis family is increasingly used as a target for cancer therapy design because it has a key role in cell growth and inhibition of cell apoptosis. Also it can be used as a biomarker for targeting cancer because it is found in almost all cancer but not normal cells. Our strategy was to design (computationally) a molecule to be used as survivin inhibitor. This molecule was named lead10 and was used furthermore to find (virtually) existing drugs with a good survivin inhibition activity.
Background: Hormonal changes during pregnancy have been suggested to predispose women to gingivitis. Furthermore, advance periodontal infection in pregnant women may pose a threat to the placenta and uterus and may increase the like hood of preterm delivery. The aim of this study was to investigate the effect of salivary interleukin -6 (IL-6) level and periodontal health among preterm postpartum women. Materials and Methods: Salivary samples were taken from 33 preterm postpartum women (study group) and 33 full term postpartum women (control group). The supernatant salivary samples were assayed using atomic absorption spectrophotometer. Plaque, calculus and gingival indices were used for recording the oral hygiene and gingivitis also probing
... Show MoreThe present study aims to evaluate the effects of methotrexate (MTX) with and without vitamin A (Vit. A) on some biochemical parameters and histological structure in male rabbits liver. Twenty male rabbits weighing 1250-1480 gm were divided into four equal number groups. The first group was given 2 ml distilled water as control group. The second group was given MTX (20 mg/kg), the third group was given Vit. A (5000 IU), while the fourth group was given MTX (20 mg/kg) +Vit. A (5000 IU) in alternative days. Following four weeks of treatment, lipid profile total cholesterol (TC), triglycerides (TG), high-density lipoprotein (HDL), [low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL)]; in addition to thyroid hormones tr
... Show MoreSo far synthesis of Gonadotropin Releasing Hormone (GnRH) analogues reported in the literature has clarified some aspects of structural activity of the naturally released GnRH. As a part of continuing efforts for further understanding of this relationship, the present investigation was undertaken which involved synthesis and biological evaluation of two GnRH analogues, firstly, by replacement of the amino acid L-Argenine in the 8th position at the backbone structure of the natural hormone by the amino acid D-Alanine; and secondly, by replacement of the amino acid L-Glycine in the 10th position by D-Alanine also at the backbone structure of the nature hormone, to obtain the following analogues respectively:
P
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