Mohammad Ali Ebrahimzadeh, Soheila Ebrahimi, Fereshteh Pourmorad,
Volume 23, Issue 107 (12-2013)
Abstract
Background and purpose: Dihydropyrimidins are bioisoester of dihydropyridine. In addition to
blocking of calcium channels, they have antimicrobial, antiviral, antifungal, antiparasital and antiinflammatory
activities. Monastrol is an anticancer dihydropyrimidine derivation that inhibits mitosis.
Several marine alkaloids with dihydropyrimidine skeletal have been isolated. In this study, several
compounds with dihydropyrimidines skeletal were prepared by reaction of imidazole aldehyde, urea and
β-keto ester.
Material and methods: Imidazole derivatives were synthesized by the reaction of the starting
materials, methyl amine hydrochloride and dihydroxyaceton dimer with potassium thiocyanate under the
reflux condition, using acetic acid and n-Butanol as solvent. In the next step, corresponding product was
methylated by methyl iodide. This product was then oxidized by MnO2 to corresponding aldehyde. The
reaction of aldehyde, urea and β-ketoester (methyl, ethyl, propyl and butyl acetoacetate) in the presence
of Lewis acid, gave the final products.
Results: The yields were 50 to 70%. The structure of all products was confirmed by analytical
methods such as NMR, IR and Mass spectra.
Conclusion: Changing the solvent of a reaction is one method for increasing the yield of
reaction. In this study, acid acetic was used as solvent instead of ethanol. The goal of this study was to
obtain the structures with antimicrobial and anti-inflammatory activities. Because of known antimicrobial
and anti-inflammatory activities of imidazolering, it seems that the combination of these two nucleuses
may create structures with improved activities.
Hossein Jalali, Ramin Shekarriz, Mohammad Reza Mahdavi,
Volume 29, Issue 173 (6-2019)
Abstract
Background and purpose: 5-Flourouracil (5-FU) is one of the most common chemical drugs used in chemotherapy of patients with cancers. Dihydropyrimidine dehydrogenase (DPD) is a critical enzyme in the catabolism of 5-FU. More than 80% of the administered 5-FU is catabolized by DPD. c.1905+1G>A mutation on DPD gene is the most important mutation associated with DPD enzymatic deficiency which leads to toxicity. The aim of this study was to investigate the frequency of c.1905+1G>A mutation on DPD gene among patients with colorectal cancer in Mazandaran province, north of Iran, 2016.
Materials and methods: In this descriptive study, 60 patients with colorectal cancer were selected and the genomic DNA was extracted from 200 µl of peripheral blood using commercial DNA extraction kit (Yekta Tajhiz Iran). For identification of c.1905+1G>A mutation on DPYD gene PCR-RFLP method was used applying Mae II restriction enzyme.
Results: The patients were 26 females and 34 males. The c.1905+1G>A mutation was detected only in one male subject (1.6%) in the heterozygous state.
Conclusion: The present study showed low frequency of c.1905+1G>A mutation in Mazandaran province. However, genetic test is recommended for identification of this mutation in oredr to predict the toxicity of the 5-FU in patients with colorectal cancer.