Ispitivanje antiproliferativne aktivnosti novih derivata benzotiazolamina prema MCF-7 ćelijskoj liniji humanog kancera dojke

Abstract

Poznato je da se mnogi lekovi, derivati benzotiazola, vrlo uspešno koriste u tretmanu različitih kliničkih stanja.1 Takođe, značajno mesto zauzimaju u istraživanjima antitumorskih agenasa i veliki broj strukturnih modifikacija jezgra benzotiazola načinjen je s ciljem poboljšanja njihove antitumorske aktivnosti. U okviru naših istraživanja u ovoj oblasti sintetisana je serija novih karbamata i amida 6-alkiltio-supstituisanih benzotiazolamina i ispitana je njihova antiproliferativna aktivnost prema MCF-7 ćelijskoj liniji humanog karcinoma dojke. Pokazano je da derivati benzotiazolamina izazivaju visoko specifičnu programiranu ćelijsku smrt apoptozu u značajnom procentu tretiranih MCF-7 ćelija. Ispitan je i uticaj novih jedinjenja na ćelijski ciklus, mitohondrijski membranski potencijal i nivo unutarćelijskih reaktivnih kiseoničnih vrsta

Numerous benzothiazole-based clinical drugs have been extensively used in practice to treat various type of diseases with high therapeutic efficacy.1 In addition, benzothiazole derivatives are compounds of an undoubted interest in anticancer research and a lot of structural modifications on their core nuclei have been made to improve their antitumor activety. Therefore, we have synthesized a series of novel 6-alkylthio-substituted benzothiazolamine carbamates and amides. To investigate their anticancer potency, we have used MCF7 human breast cancer cell line. Benzothiazolamine derivatives show great potency for promoting highly specific programmed cell death apoptosis in MCF-7 cancer cell line. Our research continued towards examination of our compounds influence on cell cycle phase distribution, reactive oxygen species level and mitochondrial membrane potential.