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.
Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu
... Show MoreBreast cancer is the second most common cancer in women world. Multiple Cytokines appear to have a dominant role in human breast cancer formation. Estimation of the in situ expression of IL-6 and IL-1β in breast cancer patients. A sixty patients with breast cancer BC were divided into two clinical subgroups, (30) with malignant breast cancer MBC and (30) with benign breast tumor as a control group according to histological examination. In situ hybridization technique used for detection of IL-6 and IL-1β mRNA sequence in two groups. The results showed that percentages of mRNA expression of IL-6 and IL-1β were in (≥ 11-50%) for malignant breast cancer. This research also investigated that (73.3%) of beni
... Show MoreA novel series of liquid crystalline compounds containing 2,4-thiazolidinedione units with varying terminal alkyl chain lengths was successfully synthesized and characterized. The chemical structures of the synthesized compounds were confirmed by FT-IR, ¹H-NMR, and mass spectrometry. The mesomorphic behavior was investigated using polarized optical microscopy (POM) and differential scanning calorimetry (DSC). Compounds [V]₄, [V]₅, and [V]₆ exhibited enantiotropic nematic phases, while compound [V]₈ displayed a smectic A (SmA) phase. No liquid crystalline behavior was observed for compound [V]₃. The liquid crystalline properties were found to depend on the terminal-to-lateral chain length ratio, molecular geometry, and the nature
... Show MoreBackground: Acute appendicitis is the most common surgical abdominal emergency with a life time prevalence of 1 to 7 individuals. Because the clinical diagnosis of acute appendicitis remains a challenge to surgeons, so different aids were introduced like different scoring systems, computer aided programs, ultrasonography, computerized tomography, Magnetic resonance imaging, Gastrointestinal tract contrast studies and laparoscopy to improve the diagnostic accuracy.
Objective: To evaluate ultrasound in the diagnosis of acute appendicitis in those patients clinically diagnosed with histopathology as gold standard.
Methods: A cross sectional study carried in Al-kindy Teaching
... Show MoreThis work includes the synthesis of new ester compounds containing two 1,3,4-oxadiazole rings, 15a-c and 16a-c. This was done over seven steps, starting with p-acetamido-phenol 1 and 2-mercaptobenzoimidazole 2. The structure of the products was determined using FT-IR, 1H NMR, and mass spectroscopy. The evaluation of the antimicrobial activities of some prepared compounds was achieved against four types of bacteria (two types of gram-positive bacteria; Staphylococcus aureus and Bacillus subtilis, and two types of gram-negative bacteria, Pseudomonas aeruginosa and E. Coli), as well as against one types of fungus (C. albino). The results show moderate activit against the study bacteria, and the theoretical analysis of the toxi
... Show MoreAsthma is a chronic respiratory disorder in which immunological and structural cells play a role. The limits of conventional medicines necessitate the development of innovative therapeutic techniques for asthma. In the present study, we investigated the possible protective effect of cinnamic acid (CA) on ovalbumin-induced asthma in a mouse model. Sixty albino male mice BALB/c type weighing (20-30) grams were chosen at random and divided into five groups each one contains 12 animal: Group I: PBS/liquid paraffin control. Group II: asthma model group. Group III: cinnamic acid control group; mice received cinnamic acid (50 mg/kg) in liquid paraffin orally by gavage. Group IV: asthma model / group of (25 mg / kg) cinnamic acid; mice received
... Show MoreCiprofloxacin, which is a second generation of fluoroquinolone and one of the most effective and widely used drugs within fluoroquinolone. Unfamiliar adverse effects of ciprofloxacin such as bone marrow (BM) suppression, thrombocytopenia, anemia, agranulocytosis, renal failure, and others observed. Lutein, is a xanthophyll (an oxygenated carotenoid), was focused by most studies as it has a strong antioxidant activity in vitro; and also, it has been associated with reducing the risk of the age-related disorders. The current study was designed to describe the role of apoptosis through the measurement of Bcl-2 associated X protein (Bax) marker, as mechanisms of bone marrow toxicity induced by ciprofloxacin and to find whether lutei
... Show MoreCiprofloxacin is widely used in treating adults infected with Gram-negative bacteria. It is contraindicated in children, growing adolescents and during pregnancy due to joint toxicity. Its toxicity concerning other organs needs to be clarified. Thus, this study was designed to study the possible cardiac damage induced by two selected doses of ciprofloxacin in juvenile rats.Eighteenth healthy juvenile rats (4 weeks old and their weight 30 ± 2 gm) were utilized in this study and divided into three groups. Group-I control; group II and group III, respectively injected IP with 25 mg/kg and 50 mg/kg ciprofloxacin every 12 hours for one week. Serum enzymes activities alanine aminotransferase (ALT), aspartate aminotransferase (AST), cr
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