Title :

Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on isocombretastatin A-4.

Author(s) :

Lamaa, D. [Auteur]
Lin, H. P. [Auteur]
Zig, L. [Auteur]
Bauvais, C. [Auteur]
Bollot, G. [Auteur]
Bignon, J. [Auteur]
Levaique, H. [Auteur]
Pamlard, Olivier [Auteur]
Dubois, J. [Auteur]
Ouaissi, M. [Auteur]
Souce, M. [Auteur]
Kasselouri, A. [Auteur]
Saller, F. [Auteur]
Borgel, D. [Auteur]
Jayat-Vignoles, C. [Auteur]
Al-Mouhammad, H. [Auteur]
Feuillard, J. [Auteur]
Benihoud, K. [Auteur]
Alami, M. [Auteur]
Hamze, A. [Auteur]

Journal title :

J. Med. Chem.

Abbreviated title :

J. Med. Chem.

Publication date :

2018-07-13

ISSN :

1520-4804

HAL domain(s) :

Chimie

English abstract : [en]

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 ...
Show more >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.Show less >

Language :

Anglais

Administrative institution(s) :

Université de Lille
CNRS
Centrale Lille
ENSCL
Univ. Artois

Collections :

• Unité de Catalyse et Chimie du Solide (UCCS) - UMR 8181

Submission date :

2023-05-30T16:02:38Z