posted on 2018-07-13, 00:00authored byDiana Lamaa, Hsin-Ping Lin, Lena Zig, Cyril Bauvais, Guillaume Bollot, Jérôme Bignon, Helene Levaique, Olivier Pamlard, Joelle Dubois, Mehdi Ouaissi, Martin Souce, Athena Kasselouri, François Saller, Delphine Borgel, Chantal Jayat-Vignoles, Hazar Al-Mouhammad, Jean Feuillard, Karim Benihoud, Mouad Alami, Abdallah Hamze
Designing
multitarget drugs have raised considerable interest due to their advantages
in the treatment of complex diseases such as cancer. Their design
constitutes a challenge in antitumor drug discovery. The present study
reports a dual inhibition of tubulin polymerization and HDAC activity.
On the basis of 1,1-diarylethylenes (isoCA-4) and
belinostat, a series of hybrid molecules was successfully designed
and synthesized. In particular compounds, 5f and 5h were proven to be potent inhibitors of both tubulin polymerization
and HDAC8 leading to excellent antiproliferative activity.