Створення бібліотеки N-(2,4-діарилтіазол-5-іл)бензамідинів та вплив цих сполук на ріст ракових клітин

• Datum: 2022
• Автори та афіліації: Oleksandr O. Severin — V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine; Maryna V. Kachaeva — V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine; Stepan G. Pilyo — V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine; Olga V. Shablykina — V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine; Taras Shevchenko National University of Kyiv, Kyiv, Ukraine; Viktoriia S. Moskvina — V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine; Taras Shevchenko National University of Kyiv, Kyiv, Ukraine; Volodymyr S. Brovarets — V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Kyiv, Ukraine
• Ключові слова: keywords
• Hauptverfasser: Severin, Oleksandr O., Kachaeva, Maryna V., Pilyo, Stepan G., Shablykina, Olga V., Moskvina, Viktoriia S., Brovarets, Volodymyr S.
• Format: Artikel
• Sprache: Englisch
• Veröffentlicht: V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2022
• Schlagworte: N-(2,4-діарилтіазол-5-іл)бензамідини; комбінаторна бібліотека; антиракова активність
• Online Zugang: https://bioorganica.com.ua/index.php/journal/article/view/31
• Назва журналу: Ukrainica Bioorganica Acta

A versatile and efficient protocol for the synthesis of library of N-(2,4-diarylthiazol-5-yl)benzamidines is described. We obtained a library of 25 diversity with different of substituents in four positions in key framework. The synthesized amidine derivatives were evaluated for their in vitro anticancer activity. Analysis of anticancer activity on 60 cancer cell lines showed a decrease of proliferation of Colon Cancer and Leukemia cell lines by more than half and allowed to establish the structure-activity relationship.