Title
Discovery of novel (imidazo[1,2-a]pyrazin-6-yl)ureas as antiproliferative agents targeting p53 in non-small cell lung cancer cell lines
Date Issued
01 April 2016
Access level
metadata only access
Resource Type
journal article
Author(s)
Bazin M.A.
Rousseau B.
Marhadour S.
Tomasoni C.
Evenou P.
Piessard S.
Ruchaud S.
Bach S.
Roussakis C.
Marchand P.
Publisher(s)
International Institute of Anticancer Research
Abstract
A series of (imidazo[1,2-a]pyrazin-6-yl)ureas were synthesized through 6-aminoimidazo[1,2-a]pyrazine as a key intermediate. 1-(Imidazo[1,2-a]pyrazin-6-yl)-3-(4-methoxy-phenyl)urea displayed a cytostatic activity against a nonsmall cell lung cancer cell line and was chosen for further mechanistic studies. Growth kinetics highlighted a selective dose-dependent response of P53-mutant NSCLC-N6-L16 cell line and overexpression of TP53 gene induced by this compound. These pharmacological data suggest a promising reactivation of p53 mutant in NSCLC-N6-L16 cell line.
Start page
1621
End page
1630
Volume
36
Issue
4
Language
English
OCDE Knowledge area
Oncología
Farmacología, Farmacia
Subjects
Scopus EID
2-s2.0-84984533425
PubMed ID
Source
Anticancer Research
ISSN of the container
02507005
Sources of information:
Directorio de Producción Científica
Scopus