A postcolumn derivatization reversed-phase high-pressure liquid chromatography method has been developed to detect and separate the one-ring open intermediates of dexrazoxane (ICRF-187) in blood plasma. Dexrazoxane is clinically used as a doxorubicin cardioprotective agent and may act by preventing iron-based oxygen-free radical damage through the iron-chelating ability of its one-ring open int...

PURPOSE Although single nucleotide polymorphisms (SNP) of the dihydropyrimidine dehydrogenase gene (DPYD) have been reported, which affect enzyme activity and the severity of 5-fluorouracil (5-FU) toxicity, no pretherapeutic detection has thus far been developed. We investigated 22 DPYD gene SNPs, their respective incidence, their link with grade 3 to 4 toxic side effects, and their management ...

PURPOSE An efficient method has been described for synthesis of 6-(substituted aryl)-4-(3,5-diphenyl-1H-1,2,4-triazol-1-yl)-1, 6-dihydropyrimidine-2-thiol, as a beneficial antimicrobial, anticonvulsant and anticancer agents. METHODS The clalcones of title compounds were synthesized in three steps and subsequently these chalcones were further reacted with thiourea in the presence of KOH in eth...

Acute esophagitis and esophageal strictures typically occur after local radiation therapy to the thoracic field. Toxicity is usually limited to the field of radiation and potentially augmented by concomitant use of chemotherapy, however esophageal stricturing due to chemotherapy alone is exceedingly rare. Gastrointestinal toxicity has been previously reported in the setting of 5-fluorouracil (5...

Montmorillonite modified is an efficient environmental friendly catalyst under one-pot-three-component synthesis of 3,4-dihydropyrimidine-2(1H) ones. The preparation was performed with an aldehyde, 1,3-dicarbonyl compounds, urea or thiourea under solvent-free conditions. In comparison with the other methods of Biginelli reaction, this new method has short reaction time inexpensive catalyst and ...

an efficient synthesis route to 1,4-dihydropyrimidine derivatives from reaction of divergent aldehydes with ethylacetoacetate and urea under solvent-free conditions by zno nanoparticles as a relative in expansive, eco-friendly, easy available, non-volatile, non-explosion, thermally robust, recyclable and easy to handle catalyst at 90°c with excellent yields is described. unenhanced reaction tim...

Dihydropyrimidine and amidoalkyl naphthol derivatives have been prepared efficiently in a one-pot synthesis using ZnCl2/urea and ZnCl2/acetamide deep eutectic systems as reaction medium and homogeneous catalyst. This method offers some advantages such as simple procedure, inexpensive solvent and catalyst and good yields of the final products in short reaction times. The use of non-toxic and env...

The kinetic properties and control mechanisms of 5-fluorouracil (5-FU), uracil, and thymine degradation by rat liver dihydropyrimidine dehydrogenase were studied in vitro. The calculated Michaelis constant (Km) for 5-FU was 3.49 +/- 0.41 (SE) microM, similar to those for uracil (2.26 +/- 0.28 microM) and for thymine (2.23 +/- 0.34 microM). However, the reduction of 5-FU appears to be most sensi...

Incubation of 5-iodo-5,6-dihydrouracil (IH2Ura) with soluble rat liver enzymes at 37 degrees, pH 8.2, results in the rapid release of iodide ion. The second product resulting from the carbon skeleton of the dihydropyrimidine ring system is 2-amino-2-oxazoline-5-carboxylic acid (I). Ultraviolet absorbance measurements at 225 nm, where both IH2Ura and iodide ion absorb, indicate that IH2Ura dehal...

A classic example of a rationally developed class of anticancer drugs, the fluoropyrimidines are now the focus of further rational approaches to cancer chemotherapy as they are transformed into oral formulations. Given alone, oral 5-fluorouracil (5-FU) has erratic absorption and nonlinear pharmacokinetics. However, when oral 5-FU is given as a prodrug and/or paired with a dihydropyrimidine dehy...