Title :

Discovery of indolizines containing triazine moiety as new leads for the development of antitumoral agents targeting mitotic events

Author(s) :

Lucescu, Liliana [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Belei, Dalila [Auteur]
Rigo, Benoit [Auteur]
Dubois, Joelle [Auteur]
Bicu, Elena [Auteur]

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

25

Pages :

3975-3979

Publication date :

2015-09-15

ISSN :

0960-894X

English keyword(s) :

PLK1
Hilbert-Johnson transposition
O-demethylation
Polo-like kinase 1 inhibitor
Antitumor agent
Dimethoxytriazine
Indolizine

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

A new family of 3-aroylindolizines bearing a dimethoxytriazine unit in their position 1 was designed, synthesized and evaluated for their ability to inhibit tubulin polymerization and cellular growth in vitro. Compound 39 ...
Show more >A new family of 3-aroylindolizines bearing a dimethoxytriazine unit in their position 1 was designed, synthesized and evaluated for their ability to inhibit tubulin polymerization and cellular growth in vitro. Compound 39 was the best candidate in the current study with a GI50 value of 870 nM on SNB-75 CNS cancer cells and of 920 nM on MDA-MB-231/ATCC breast cancer cells. The standard NCI Compare results indicated that indolizine 39 may target PLK1 (polo-like kinase 1).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 :

2019-05-17T13:14:36Z