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Methylene versus carbonyl bridge in the ...
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Document type :
Article dans une revue scientifique
DOI :
10.1016/j.bmc.2016.09.063
PMID :
27707624
Permalink :
http://hdl.handle.net/20.500.12210/11281
Title :
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings
Author(s) :
Moise, Iuliana-Monica [Auteur]
Bicu, Elena [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Rigo, Benoit [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Journal title :
Bioorganic & medicinal chemistry
Abbreviated title :
Bioorg. Med. Chem.
Volume number :
24
Pages :
6021-6030
Publication date :
2016-11-15
ISSN :
0968-0896
English keyword(s) :
Phenothiazine
Antitumor agent
9(10H)Acridone
Iminodibenzyl
Phenoxazine
Azaphenothiazine
Tubulin inhibitor
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
The phenothiazine group has been identified as a suitable A ring in the structure of tubulin polymerization inhibitors. In our search to identify more potent inhibitors, a study of different isosteric tricyclic groups as ...
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The phenothiazine group has been identified as a suitable A ring in the structure of tubulin polymerization inhibitors. In our search to identify more potent inhibitors, a study of different isosteric tricyclic groups as new potential A rings was first realized and permitted to identify 1-azaphenothiazine and iminodibenzyl as favorable modulations providing compounds with improved activity against tubulin. An investigation of the methylene group as the connector between the A and B rings revealed that the "CH" bridge was tolerated, improving the biological potency when the A unit was of phenothiazine, 1-azaphenothiazine or iminodibenzyl type. Molecules 6-8 and 12 showed increased biological activity in comparison to parent phenstatin 2 on COLO 205 colon cancer cell line. The most antineoplastic agent in the current study was phenothiazine 5 displaying a GI of 25nM against the melanoma MDA-MB-435 cell line.Show less >
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
CHU Lille
Inserm
Université de Lille
Collections :
  • Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Research team(s) :
Therapeutic innovation targetting inflammation
Submission date :
2019-05-17T13:14:41Z
Université de Lille

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