Title :

Studies on indolizines. Evaluation of their biological properties as microtubule-interacting agents and as melanoma targeting compounds

Author(s) :

Ghinet, Alina [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Abuhaie, Cristina-Maria [Auteur]
Gautret, Philippe [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Rigo, Benoit [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Belei, Dalila [Auteur]
Bicu, Elena [Auteur]

Journal title :

European journal of medicinal chemistry

Abbreviated title :

Eur. J. Med. Chem.

Volume number :

89

Pages :

115-127

Publication date :

2015-01-07

ISSN :

0223-5234

English keyword(s) :

Indolizine
Microtubule
Melanoma
[3+2] Cycloaddition
Antitubulin
Anticancer agent
5,6-Fused bicyclic heteroaromatic

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

With the aim of investigating new analogues of phenstatin with an indolizin-3-yl unit, in particular as the B-ring, three new series of compounds (6-8, 9-34 and 54) were synthesized and tested for interactions with tubulin ...
Show more >With the aim of investigating new analogues of phenstatin with an indolizin-3-yl unit, in particular as the B-ring, three new series of compounds (6-8, 9-34 and 54) were synthesized and tested for interactions with tubulin polymerization and evaluated for cytotoxicity on an NCI-60 human cancer cell lines panel. The replacement of the 3'-hydroxy-4'-methoxyphenyl B-ring of phenstatin with substituted indolizine unit results in the conservation of both antitubulin and cytotoxic effect. Indolizines 9 and 17 were the most effective in the present study and showed the highest antiproliferative effect on melanoma cell lines MDA-MB-435 (GI50 = 30 nM) and could serve as new lead compounds for the development of anti-cancer therapeutics.Show less >

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Lille Inflammation Research International Center (LIRIC) - U995

Research team(s) :

Therapeutic innovation targetting inflammation

Submission date :

2019-05-17T13:14:34Z