Citotoksično djelovanje tieno[2,3-b]piridinskih spojeva na stanice humanog karcinoma mokraćnog mjehura

Objectives: The purpose of this study was to determine the effects of treating bladder cancer cells with the newly synthesized thieno[2,3-b]pyridine anticancer agents, by focusing on its cytotoxic effects on the investigated human cell line T24. Methods: The T24 bladder cancer cell line was treated with a newly developed thieno[2,3-b]pyridine anticancer compounds: Inhibitor 5 3-amino-N-(3-chloro-2-methylphenyl)-5-oxo-5,6,7,8-tetrahydrothieno[2,3-b]quinoline-2-carboxamide, Inhibitor 6 3-amino-N-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydrothieno[2,3-b]quinoline-2-carboxamide, Inhibitor 8 (E)-3-amino-5-(3-(3-bromophenyl)acryloyl)-N-(3-chloro-2-methylphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide and Inhibitor 9 (E)-3-amino-5-(3-(3-bromophenyl)-1-hydroxyallyl)-N-(3-chloro-2-methylphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide to determine its cytotoxic effect on T24 cells. The 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay was performed to analyze the cellular metabolic activity and determine the cytotoxic effect. Results: Inhibitors 5, 6, 8 and 9 all showed significant cytotoxic effect on the bladder cancer cells in a dose- and time-dependent manner. The most effective was Inhibitor 8 with an IC50 value of 0.4041 μg/mL after 72 hours. Conclusion: Due to their cytotoxic effect on bladder cancer cells, Inhibitors 5, 6, 8 and 9 deserve further attention as a potential treatment for transitional cell cancer.
Ciljevi: Svrha ove studije bila je utvrditi učinke tretiranja stanica raka mokraćnog mjehura novosintetiziranim tieno[2,3-b]piridin antitumorskim spojevima, fokusirajući se na njihove citotoksične učinke na ispitivanu humanu staničnu liniju T24. Materijali i metode: T24 stanična linija raka mokraćnog mjehura tretirana je novosintetiziranim tieno[2,3-b]piridin antitumorskim spojevima: Inhibitor 5 - 3-amino-N-(3-kloro-2-metilfenil)-5-okso-5,6,7,8-tetrahidrotieno[2,3-b]kinolin-2-karboksamid, Inhibitor 6 - 3-amino-N-(naftalen-1-il)-5-okso-5,6,7,8-tetrahidrotieno[2,3 -b]kinolin-2-karboksamid, Inhibitor 8 - (E)-3-amino-5-(3-(3-bromofenil)akriloil)-N-(3-klor-2-metilfenil)-6-metiltieno[2, 3-b]piridin-2-karboksamid i Inhibitor 9 - (E)-3-amino-5-(3-(3-bromofenil)-1-hidroksialil)-N-(3-klor-2-metilfenil)-6- metiltieno[2,3-b]piridin-2-karboksamid, kako bi se odredio njihov citotoksični učinak na T24 stanice. Proveden je test 3-(4,5-dimetiltiazolil-2)-2,5-difeniltetrazolij bromida (MTT) kako bi se analizirala stanična metabolička aktivnost i odredio citotoksični učinak. Rezultati: Svi inhibitori 5, 6, 8 i 9 pokazali su značajan citotoksični učinak na stanice raka mokraćnog mjehura i taj učinak je ovisan o dozi i vremenu inkubacije. Najučinkovitiji je bio Inhibitor 8 s IC50 vrijednošću od 0,4041 μg/mL nakon 72 sata. Zaključci: Zbog svog citotoksičnog učinka na stanice raka mokraćnog mjehura, Inhibitori 5, 6, 8 i 9 zaslužuju daljnju pozornost kao potencijalni tretman za rak prijelaznih stanica.