Benzothiazole carbamates and amides as antiproliferative species

A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apopto...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2018-09, Vol.157, p.1096-1114
Main Authors: Videnović, Milica, Mojsin, Marija, Stevanović, Milena, Opsenica, Igor, Srdić-Rajić, Tatjana, Šolaja, Bogdan
Format: Article
Language:English
Subjects:
Anoikis
Antiproliferative
Benzothiazoles
MCF-7
NT2/D1
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Summary:A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apoptosis, G2/M cell cycle arrest and decrease ROS level in MCF-7 human breast cancer cell line. Moreover, submicromolar antiproliferative activity of examined carbamates against NT2/D1 testicular embryonal carcinoma was shown. The most potent derivatives strongly inhibited NT2/D1 cell migration and invasiveness. [Display omitted] •New antiproliferative benzothiazole carbamates and amides are synthesized.•Benzothiazoles induce apoptosis and G2/M arrest along with ROS reduction in MCF-7 cells.•Detached NT2/D1 cells that underwent apoptosis point to anoikis.•Benzothiazole derivatives strongly inhibit migration and invasiveness of NT2/D1 cells.•The most potent compounds show no toxicity in vitro and in vivo.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2018.08.067