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Farhad Mostafavi Shahab,Simin Dadashzadeh,Farzad Kobarfard 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.10
KBF-611 is a new thiosemicarbazone derivative which has demonstrated significant antituberculosis effect. A sensitive and specific HPLC method was established and validated for the determination of KBF-611 and its deacetylated metabolite (KM) in mouse and rabbit plasma. Chromatographic separation was achieved on a Eurospher-100 C8 column using acetonitrile, methanol, phosphate buffer (pH 7) and TEA (25:5:70:0.1, v/v), as mobile phase at a flow rate of 1 mL/min. KBF-611, KM and internal standard (4-acetamido–3–chlorobenzaldehyde thiosemicarbazone) were detected at the wavelength of 323 nm. The calibration curves were linear within the concentration range from 0.02-5 μg/mL and 0.02-1 μg/mL for KBF-611 and KM respectively. The limit of detection and the limit of quantitation were 6 ng/mL and 20 ng/mL respectively for both KBF-611 and KM. The relative standard deviation for intra- and interday precision was less than 7.5%. Average recoveries were 70.8% and 75.0% for KBF-611 and KM respectively. The established HPLC method was validated to be a simple, rapid and reliable procedure and successfully applied to study the preclinical pharmacokinetics of KBF-611 and KM in mice and rabbits.
Zahra Ghiasifar,Hafezeh Salehabadi,Neda Adibpour,Eskandar Alipour,Farzad Kobarfard,Mohammad Reza Shoushizadeh 대한화학회 2021 Bulletin of the Korean Chemical Society Vol.42 No.1
In this study, a novel catalyst based on layered double hydroxides (LDHs) attached by hexamethylene-1,6-diisocyanate (HMDI) and citric acid (LDHs-g-HMDI-Citric acid) is reported and used to increase the yield of biurets synthesis. Biuret derivatives 5a?n were prepared by reaction of several phenyl allophanates (3a?d), which prepared from the reaction of phenyl chloroformate and urea derivatives (2a?d), with variously substituted amines (4a?g) in the presence of LDHs-g-HMDI-Citric acid as a reusable heterogeneous catalyst at reflux condition for 60?180?min. These biurets (5a?n) were evaluated for human immunodeficiency virus type-1 (HIV-1) protease inhibitory activity by HIV-1 p24 antigen ELISA kit and six of them (5n, 5i, 5j, 5 m, 5f, and 5a) showed moderate activity on HIV-1 virus with IC50 values ranging from 55 to 100??M compared with the azidothymidine as the reference drug (IC50 =?0.11??M). Results of the in vitro test and docking study were in good correlation.
Zahra Eskandariyan,Marjan Esfahani Zadeh,Kamaleddin Haj Mohammad Ebrahim Tehrani,Vida Mashayekhi,Farzad Kobarfard 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.3
A series of 2-(arylmethylthio)-3-phenylquinazolin-4-one derivatives have been synthesized and theirantiplatelet aggregation activities were assessed againstADP and arachidonic acid-induced platelet aggregation inhuman plasma. Among the tested thioethers, derivative 2,3, 5 and 16 were the most potent compounds with satisfactoryIC50 for inhibition of platelet aggregation inducedby ADP. Analysis of global physicochemical parametersshows some correlations between activities and molecularvolume and also surface area of the studied derivatives.
Eskandariyan, Zahra,Zadeh, Marjan Esfahani,Tehrani, Kamaleddin Haj Mohammad Ebrahim,Mashayekhi, Vida,Kobarfard, Farzad 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.3
A series of 2-(arylmethylthio)-3-phenylquinazolin-4-one derivatives have been synthesized and their antiplatelet aggregation activities were assessed against ADP and arachidonic acid-induced platelet aggregation in human plasma. Among the tested thioethers, derivative 2, 3, 5 and 16 were the most potent compounds with satisfactory $IC_{50}$ for inhibition of platelet aggregation induced by ADP. Analysis of global physicochemical parameters shows some correlations between activities and molecular volume and also surface area of the studied derivatives.
Karim Ebrahim,Farshad H. Shirazi,Hosein Vatanpour,Abas zare,Farzad Kobarfard,Hadi Rabie 한국유방암학회 2014 Journal of breast cancer Vol.17 No.4
Purpose: Breast cancer is a significant health problem worldwide,accounting for a quarter of all cancer diagnoses in women. Current strategies for breast cancer treatment are not fully effective,and there is substantial interest in the identification of novelanticancer agents especially from natural products includingtoxins. Cytotoxins are polypeptides found in the venom of cobrasand have various physiological effects. In the present study,the anticancer potential of cytotoxin-II against the human breastadenocarcinoma cell line (MCF-7) was investigated. Methods:The cytotoxic effects of cytotoxin-II were determined by morphologicalanalysis and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide assay. The mode and mechanism of celldeath were investigated via acridine orange/ethidium bromide(AO/EtBr) double staining, flow cytometric analysis of cell death,detection of mitochondrial membrane potential, measurement ofintracellular reactive oxygen species (ROS), annexin V/propidiumiodide staining, and caspase-9 activity assays. Results: The halfmaximal inhibitory concentration (IC50) of cytotoxin-II in MCF-7cells was 4.18±1.23 μg/mL, while the value for cisplatin was approximately28.02±1.87 μg/mL. Morphological analysis and AO/EtBr double staining showed typical manifestations of apoptoticcell death (in doses lower than 8 μg/mL). Dose- and time-dependentROS generation, loss of mitochondrial membrane potential,caspase-9 activation, and cell cycle arrest were observed in theirrespective tests. Conclusion: In conclusion, cytotoxin-II has potentanticancer effects in the MCF-7 cell line, which are inducedvia the intrinsic pathways of apoptosis. Based on these findings,cytotoxin-II is a suitable choice for breast cancer treatment.
Synthesis, antimycobacterial and anticancer activity of novel indole-based thiosemicarbazones
Vida Mashayekhi,Kamaleddin Haj Mohammad Ebrahim Tehrani,Parisa Azerang,Soroush Sardari,Farzad Kobarfard 대한약학회 2021 Archives of Pharmacal Research Vol.44 No.8
Based on the structural elements of bioactiveindole-based compounds, a series of novel 1-substitutedindole-3-carboxaldehyde thiosemicarbazones were synthesizedas potential antimycobacterial and anticancer agents. The derivatives were prepared via a two-step methodologyincluding N-alkylation(benzylation) of indole-3-carboxaldehydeand conversion of the intermediate aldehydes tocorresponding thiosemicarbazones. The derivatives wereevaluated for their antimycobacterial activity and compounds3d (R = propyl) and 3q (R = 4-nitrobenzyl) wereamong the most potent and selective derivatives with IC50values of 0.9 and 1.9 lg/mL respectively. The anticanceractivity of the derivatives was also assessed against a panelof tumor cell lines. Compounds 3t, 3u, 3v and 3w efficiently inhibited the majority of the cancer cell lineswith considerable selectivity.
Nadia Kalhor,Matin Mardani,Sepideh Abdollahzadeh,Mona Vakof,Marjan Esfahani Zadeh,Kamaleddin Haj Mohammad Ebrahim Tehrani,Farzad Kobarfard,Shohreh Mohebbi 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.11
Based on our previous studies on antiplatelet hydrazone derivatives, some new indole-based derivatives were designed and synthesized as potential antiplatelet agents. Synthesis of the derivatives was accomplished by substitution at the N – 1 position of indole-3-carboxaldehyde and reacting the resulting intermediates with either phenylhydrazine of benzoylhydrazide. The structure of the synthesized compounds was confirmed by different spectral methods such as mass spectrometry,1H-NMR, and IR spectroscopy. The derivatives were tested for their ability to inhibit human platelet aggregation, where arachidonic acid (AA), adenosine diphosphate ADP, and collagen were used as aggregation inducers. Compounds (2a–2f) showed considerable activity against AA-induced platelet aggregation. Among them, compounds 2a, 2b, and 2f were the most potent derivatives with IC50 values comparable to that of aspirin as standard drug. Analysis of structure–activity relationship shows that with increased bulk of the substituents at indole N – 1, the antiplatelet activity is reduced, thus suggesting that steric hindrance at this position plays a major role in the activity of the tested compounds.