Cинтез та протипухлинна активність 5-сульфонільних похідних 1,3-оксазол-4-карбоксилатів

Cинтез та протипухлинна активність 5-сульфонільних похідних 1,3-оксазол-4-карбоксилатів

A series of new 2-aryl 5-sulfonyl-1,3-oxazole-4-carboxylates for NCI anticancer screening protocol against 60 cancer cell lines were synthesized. Screening was performed in vitro on 60 cell lines of lungs, kidneys, CNS, ovaries, prostate, and breast cancer, leukemia, and melanoma. Methyl 5-benzylsul...

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Datum:2020
Hauptverfasser: Pilyo, Stepan G., Kozachenko, Оlexandr P., Zhirnov, Victor V., Kachaeva, Maryna V., Kobzar, Oleksandr L., Vovk, Andriy I., Brovarets, Volodymyr S.
Format: Artikel
Sprache:English
Veröffentlicht: V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2020
Schlagworte:
5-сульфоніл-1,3-оксазол-4-карбоксилати
синтез
протипухлинна активність
селективність
молекулярний докінг
Online Zugang:https://bioorganica.com.ua/index.php/journal/article/view/36
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Назва журналу:Ukrainica Bioorganica Acta

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Ukrainica Bioorganica Acta
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Zusammenfassung:A series of new 2-aryl 5-sulfonyl-1,3-oxazole-4-carboxylates for NCI anticancer screening protocol against 60 cancer cell lines were synthesized. Screening was performed in vitro on 60 cell lines of lungs, kidneys, CNS, ovaries, prostate, and breast cancer, leukemia, and melanoma. Methyl 5-benzylsulfonyl-2-phenyl-1,3-oxazole-4-carboxylate 15 exhibited potent and broad range of cytotoxic activity against tested human cancer cells with average GI50, TGI, and LC50 values of 5.37·10-6, 1.29·10-5 and 3.6·10-5 mol/L respectively. Molecular docking was used to evaluate the possible interaction of compound 15 with tubulin as well as a complex formation with CDK2

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