Hydroxypyridinone Derivatives: Synthesis And Cytotoxic Evaluation
Journal Title: Journal of Reports in Pharmaceutical Sciences - Year 2013, Vol 2, Issue 1
Abstract
A series of 3-hydroxypyridin-4-one derivatives (HPOs) as bidentate iron (III) chelating agents were synthesized from 3-hydroxypyran-4-ones (maltol and ethyl maltol) in three steps through protection of hydroxyl group. The protected compounds were then reacted with suitable primary amines to give benzylated pyridinones. Finally, the benzyl group was removed by catalytic hydrogenation to produce the desired products. The partition coefficient of the free ligands and their iron (III) complexes were determined in an aqueous/octanol system using shake-flask method. The cytotoxic effects of these iron chelators against MCF-7 and MDA-MB-231 cancer cells were also evaluated using MTT assay. The results revealed that cytotoxicity of synthesized compounds were closely related to the lipophilycity of them so that the most lipophilic compound (4f) showed the highest activity; whereas compound 4a as a more hydrophilic agent showed the lowest cytotoxic effect; Although these compounds were cytotoxic at high concentration (≥ 0.1 mM)
Chemical composition and general toxicity of essential oil extracted from the stalks and flowers of Rheum ribes L. growing in Iran
The composition of the essential oil from the stalks and flowers of Rheum ribes L., growing in Iran, were extracted by hydrodistillation and analyzed by GC-MS. Thirty constituents representing 93.84% of Rheum oil were id...
Design, Formulation and Evaluation of Its Physiochemical Properties of Acetaminophen, Ibuprofen and Caffeine as Effervescent Tablet
The aim of this study was to design, formulate and evaluate the physicochemical properties of acetaminophen, ibuprofen and caffeine as effervescent tablets, since, they can overcome the problems with drug swallowing for...
Design, Formulation and Physicochemical Evaluation of Acetaminophen Effervescent Tablets
Background: The main objective of this study was to design, formulate and evaluate the physicochemical properties of 500 mg acetaminophen effervescent tablets, in order to accelerate its analgesic and antipyretic effects...
Effect of Streptokinase on Short-term Outcomes in the Acute Myocardial Infarction with ST-Segment Elevation
Acute coronary syndrome is one of the most prevalent cardiovascular diseases. The acute myocardial infarction is one of its kinds which embodies the indication of fibrinolysis. One of the fibrinolytic types mostly used i...
Hypoglycemic Effect of Hydroalcoholic Extract and Hexane Fraction of Persian Shallot (Allium Hirtifolium Boiss) Extract in Streptozotocin-Induced Diabetic Rats
The present study was aimed to evaluate the hypoglycemic and potential insulinotropic effects of hydroalcoholic extract and hexane fraction of Persian shallot on streptozotocin (STZ) induced diabetic rats. Forty nine mal...