Synthesis and biological evaluation of ...
Type de document :
Article dans une revue scientifique
PMID :
URL permanente :
Titre :
Synthesis and biological evaluation of thiophene and benzo[b]thiophene analogs of combretastatin A-4 and isocombretastatin A-4: A comparison between the linkage positions of the 3,4,5-trimethoxystyrene unit
Auteur(s) :
Cong, Viet Do [Auteur]
Faouzi, Abdelfattah [Auteur]
Barette, Caroline [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Fauvarque, Marie-Odile [Auteur]
Colomb, Evelyne [Auteur]
Catry, Laura [Auteur]
Berthier-Vergnes, Odile [Auteur]
Haftek, Marek [Auteur]
Barret, Roland [Auteur]
Lomberget, Thierry [Auteur]
Faouzi, Abdelfattah [Auteur]
Barette, Caroline [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Fauvarque, Marie-Odile [Auteur]
Colomb, Evelyne [Auteur]
Catry, Laura [Auteur]
Berthier-Vergnes, Odile [Auteur]
Haftek, Marek [Auteur]
Barret, Roland [Auteur]
Lomberget, Thierry [Auteur]
Titre de la revue :
Bioorganic & Medicinal Chemistry Letters
Nom court de la revue :
Bioorg. Med. Chem. Lett.
Numéro :
26
Pagination :
174-180
Date de publication :
2016-01-01
ISSN :
0960-894X
Mot(s)-clé(s) en anglais :
Antiproliferative agents
Heterocycles
Inhibitors of tubulin assembly
Combretastatin A-4
Melanocyte
Heterocycles
Inhibitors of tubulin assembly
Combretastatin A-4
Melanocyte
Discipline(s) HAL :
Sciences du Vivant [q-bio]
Résumé en anglais : [en]
Combretastatin A-4 and isocombretastatin A-4 derivatives having thiophenes or benzo[b]thiophenes instead of the B ring were prepared and evaluated for their in cellulo tubulin polymerization inhibition (TPI) and antiproliferative ...
Lire la suite >Combretastatin A-4 and isocombretastatin A-4 derivatives having thiophenes or benzo[b]thiophenes instead of the B ring were prepared and evaluated for their in cellulo tubulin polymerization inhibition (TPI) and antiproliferative activities. The presence of the benzo[b]thiophene ring proved to have a crucial effect as most of the thiophene derivatives, except those having one methoxy group, were inactive to inhibit tubulin polymerization into microtubules. The influence of the attachment position was also studied: benzo[b]thiophenes having iso or cis 3,4,5-trimethoxystyrenes at position 2 were 12-30-fold more active than the 3-regioisomers for the TPI activity. Some of the novel designed compounds exhibited interesting anti-proliferative effects on two different cell lines.Lire moins >
Lire la suite >Combretastatin A-4 and isocombretastatin A-4 derivatives having thiophenes or benzo[b]thiophenes instead of the B ring were prepared and evaluated for their in cellulo tubulin polymerization inhibition (TPI) and antiproliferative activities. The presence of the benzo[b]thiophene ring proved to have a crucial effect as most of the thiophene derivatives, except those having one methoxy group, were inactive to inhibit tubulin polymerization into microtubules. The influence of the attachment position was also studied: benzo[b]thiophenes having iso or cis 3,4,5-trimethoxystyrenes at position 2 were 12-30-fold more active than the 3-regioisomers for the TPI activity. Some of the novel designed compounds exhibited interesting anti-proliferative effects on two different cell lines.Lire moins >
Audience :
Internationale
Vulgarisation :
Non
Établissement(s) :
CHU Lille
Inserm
Université de Lille
Inserm
Université de Lille
Équipe(s) de recherche :
Therapeutic innovation targetting inflammation
Date de dépôt :
2019-05-17T13:14:36Z