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Research in Pharmaceutical Sciences، جلد ۱۹، شماره ۲، صفحات ۲۳۸-۲۵۰
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چکیده فارسی مقاله
کلیدواژه‌های فارسی مقاله
عنوان انگلیسی Molecular docking and synthesis of N-alkyl-isatin-3-imino aromatic amine derivatives and their antileishmanial and cytotoxic activities
چکیده انگلیسی مقاله Background and purpose: Isatin derivatives have excited attention due to their biological attractions, especially, anticancer properties. Isatin analogs such as semaxanib and sunitinib were exposed to tyrosine kinase inhibitory properties. N-substituted isatins were reported to show cytotoxic activity. On the other, the extension of impressive and cost-effective agents against leishmaniasis is necessary in third-world countries. The capability of isatin derivatives to create novel anticancer and anti-leishmanial compounds has been identified in medicinal chemistry research. The current study aimed to synthesize N-alkyl-isatin-3-imino aromatic amine compounds and evaluate their biological effects. Experimental approach: Synthesis started with the formation of 2-chloro-N-phenylacetamide derivatives                 by the reaction of aniline derivatives with chloroacetyl chloride. N-alkylation of isatin was performed                              in the presence of K2CO3 in N, N-dimethylformamide. Final products were prepared via the condensation                 of N-alkyl isatin derivatives with aromatic amines. Cell viability was checked out by using the MTT                          assay against cancer cells. Final compounds were screened for anti-leishmanial activity. The molecules were docked in the active sites of the epidermal growth factor receptor tyrosine kinase to define the possible interactions. Findings/Results: Compounds 5c and 4d with IC 50 value of 50 µM showed cytotoxic activity on the                            MCF-7 cell line. Compound 5b presented anti-leishmanial activity against promastigote form after 48 h (IC 50 :59 µM) and 72 h (IC 50 : 41 µM) incubations. The highest docking score was -7.33 kcal/mol for                  compound 4d. Conclusions and implications: The nature of substitution in the N1 region of isatin seems to be able to influence the cytotoxic activity. Based on the obtained results of docking and cytotoxic tests, compound 4d seems to be a good compound for further investigations.    
کلیدواژه‌های انگلیسی مقاله Anti-leishmanial activity,Cytotoxicity,Isatin,Schiff base.
نویسندگان مقاله | Farshid Hassanzadeh
Skin Disease and Leishmaniasis Research Center, Department of Parasitology and Mycology, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran.


| Seyed Hossein Hejazi
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran. Bioinformatics Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Elham Jafari
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Atefeh Mohammadi fard
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Hojjat Sadeghi-aliabadi


نشانی اینترنتی http://rps.mui.ac.ir/index.php/jrps/article/view/2246
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زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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