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- Title
Preparation and biological evaluation of new antimicrotubule agents: Modification of the imidazolidin‐2‐one moiety of phenyl 4‐(2‐oxoimidazolidin‐1‐yl)benzenesulfonates.
- Authors
Gagné‐Boulet, Mathieu; Bouzriba, Chahrazed; Chavez Alvarez, Atziri Corin; Fortin, Sébastien
- Abstract
We prepared and biologically evaluated 32 novel molecules named phenyl 4‐(dioxoimidazolidin‐1‐yl)benzenesulfonates (PID‐SOs) and ethyl 2‐(3‐(4‐(phenoxysulfonyl)phenyl)ureido)acetates (EPA‐SOs). The antiproliferative activity of PID‐SOs and EPA‐SOs was assessed on four cancer cell lines (HT‐1080, HT‐29, M21, and MCF7). The most potent PID‐SOs bearing an imidazolidin‐2,4‐dione group show antiproliferative activity in the nanomolar to low micromolar range (0.066 – 6 µM) while EPA‐SOs and PID‐SOs bearing an imidazolidin‐2,5‐dione moiety are mostly not active, exhibiting antiproliferative activity over 100 µM. The most potent PID‐SOs (16–18) arrest the cell cycle progression in G2/M phase and interact with the colchicine‐binding site leading to the microtubule and cytoskeleton disruption. Moreover, their antiproliferative activity is not impaired in vinblastine‐, paclitaxel‐, and multidrug‐resistant cell lines. Finally, our study confirms that PID‐SOs bearing the imidazolidin‐2,4‐dione moiety are a new family of promising antimitotics.
- Subjects
BENZENESULFONATES; MOIETIES (Chemistry); CELL cycle; CELL lines; CANCER cells; TUBULINS; MICROTUBULES; PACLITAXEL
- Publication
Chemical Biology & Drug Design, 2022, Vol 99, Issue 2, p187
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13971