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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.
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.
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.