کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1231290 1495254 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
DNA binding properties and biological evaluation of dihydropyrimidinones derivatives as potential antitumor agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
DNA binding properties and biological evaluation of dihydropyrimidinones derivatives as potential antitumor agents
چکیده انگلیسی


• Dihydropyrimidinones derivatives, EMPD and EMCD are efficiently synthesized.
• EMPD and EMCD are intercalative binding into CT-DNA helix.
• The binding interactions are predominantly enthalpy driven.
• EMPD and EMCD can effectively inhibit the growth of BEL-7402 and PC-12 cell lines.

The binding properties of two medicinally important dihydropyrimidinones derivatives 5-(Ethoxycarbonyl)-6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one (EMPD) and 5-(Ethoxycarbonyl)-6-methyl-4-(4-chlorophenyl)-3,4-dihydropyrimidin-2(1H)-one (EMCD) with calf-thymus DNA (ctDNA) were investigated by spectroscopy, viscosity, isothermal titration calorimetry (ITC) and molecular modeling techniques. Simultaneously, their biological activities were evaluated with MTT assay method. The binding constants determined with spectroscopic titration and ITC were found to be in the same order of 104 M−1. According to the results of viscosity studies, fluorescence competitive binding experiment and ITC investigations, intercalative binding was evaluated as the dominant binding modes between the two compounds and ctDNA. Furthermore, the results of molecular modeling corroborated those obtained from spectroscopic, viscosimetric and ITC investigations. Evaluation of the antitumor activities of the two derivatives against different tumor cell lines proved that they exhibited significant tumor cell inhibition rate, accordingly blocking DNA transcription and replication. The present results favor the development of potential drugs related with dihydropyrimidinones derivatives in the treatment of some diseases.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy - Volume 114, October 2013, Pages 214–219
نویسندگان
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