Studies on indolizines. Evaluation of their ...
Document type :
Article dans une revue scientifique
PMID :
Permalink :
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 - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Abuhaie, Cristina-Maria [Auteur]
Gautret, Philippe [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Belei, Dalila [Auteur]
Bicu, Elena [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Abuhaie, Cristina-Maria [Auteur]
Gautret, Philippe [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
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
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 >
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
Inserm
Université de Lille
Research team(s) :
Therapeutic innovation targetting inflammation
Submission date :
2019-05-17T13:14:34Z