Title :

Combretastatin a-4 sulfur-containing heterocyclic derivatives: synthesis, antiproliferative activities and molecular docking studies

Author(s) :

Faouzi, Abdelfattah [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Arnaud, Alexandre [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Bancet, Alexandre [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Barette, Caroline [Auteur]
Laboratoire de Biologie à Grande Échelle [BGE - UMR S1038]
Preto, Jordane [Auteur]
Centre de Recherche en Cancérologie de Lyon [UNICANCER/CRCL]
Do, Cong Viet [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Jordheim, Lars Petter [Auteur]
Centre Léon Bérard [Lyon]
Université Claude Bernard Lyon 1 [UCBL]
Centre de Recherche en Cancérologie de Lyon [UNICANCER/CRCL]
Bousfiha, Zineb [Auteur]
Centre Léon Bérard [Lyon]
Centre de Recherche en Cancérologie de Lyon [UNICANCER/CRCL]
Nguyen, Thi Thanh Binh [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Verriere, Marion [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Farce, Amaury [Auteur]
Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Fauvarque, Marie-Odile [Auteur]
Laboratoire de Biologie à Grande Échelle [BGE - UMR S1038]
Barret, Roland [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Santé Lyon Est - Louis Léopold Ollier
Lomberget, Thierry [Auteur]
Molécules bioactives et chimie médicinale [B2MC]
Institut de Chimie et Biochimie Moléculaires et Supramoléculaires [ICBMS]
Santé Lyon Est - Louis Léopold Ollier

Journal title :

European Journal of Medicinal Chemistry

Abbreviated title :

Eur J Med Chem

Volume number :

215

Pages :

113275

Publication date :

2021-02-08

ISSN :

1768-3254

Keyword(s) :

Heterocycles
Antiproliferative agents
Cancer
Combretastatin A-4
Inhibitors of tubulin assembly

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

Combretastatin A-4 inspired heterocyclic derivatives were synthesized and evaluated for their biological activities on tubulin polymerization and cell proliferation. Among the 19 described sulfur-containing compounds, ...
Show more >Combretastatin A-4 inspired heterocyclic derivatives were synthesized and evaluated for their biological activities on tubulin polymerization and cell proliferation. Among the 19 described sulfur-containing compounds, derivatives (Z)-4h and (Z)-4j exhibited interesting in cellulo tubulin polymerization inhibition and antiproliferative activities with IC50 values for six different cell lines between 8 and 27 nM. Furthermore, in silico docking studies within the colchicine/CA-4 binding site of tubulin were carried out to understand the interactions of our products with the protein target. The effects on the cell cycle of follicular lymphoma cells were also investigated at 1–10 nM concentrations showing that apoptotic processes occurred.Show less >

Language :

Anglais

Peer reviewed article :

Oui

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286

Submission date :

2021-07-06T12:50:15Z
2024-03-04T08:53:36Z