Discovery of novel (imidazo[1,2-a]pyrazin-6-yl)ureas as antiproliferative agents targeting p53 in non-small cell lung cancer cell lines

Marc Antoine Bazin; Bénédicte Rousseau; Sophie Marhadour; Christophe Tomasoni; Pierre Evenou; Sylvie Piessard; Abraham J. Vaisberg; Sandrine Ruchaud; Stéphane Bach; Christos Roussakis; Pascal Marchand

Discovery of novel (imidazo[1,2-a]pyrazin-6-yl)ureas as antiproliferative agents targeting p53 in non-small cell lung cancer cell lines

Marc Antoine Bazin
, Bénédicte Rousseau
, Sophie Marhadour
, Christophe Tomasoni
, Pierre Evenou
, Sylvie Piessard
, Abraham J. Vaisberg
, Sandrine Ruchaud
, Stéphane Bach
, Christos Roussakis
, Pascal Marchand

School of Science and Engineering

UFR des Sciences Pharmaceutiques et Biologiques
Pierre and Marie Curie University Paris 06

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

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.

Original language	English
Pages (from-to)	1621-1630
Number of pages	10
Journal	Anticancer Research
Volume	36
Issue number	4
State	Published - Apr 2016

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antiproliferative activity
Imidazo[1,2-A]pyrazine
NSCLC
P53
Urea

Cite this

@article{526eec61df844bb4a6e2899dc7e68450,

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",

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.",

keywords = "Antiproliferative activity, Imidazo[1,2-A]pyrazine, NSCLC, P53, Urea",

author = "Bazin, \{Marc Antoine\} and B{\'e}n{\'e}dicte Rousseau and Sophie Marhadour and Christophe Tomasoni and Pierre Evenou and Sylvie Piessard and Vaisberg, \{Abraham J.\} and Sandrine Ruchaud and St{\'e}phane Bach and Christos Roussakis and Pascal Marchand",

year = "2016",

month = apr,

language = "Ingl{\'e}s",

volume = "36",

pages = "1621--1630",

journal = "Anticancer Research",

issn = "0250-7005",

number = "4",

}

TY - JOUR

T1 - Discovery of novel (imidazo[1,2-a]pyrazin-6-yl)ureas as antiproliferative agents targeting p53 in non-small cell lung cancer cell lines

AU - Bazin, Marc Antoine

AU - Rousseau, Bénédicte

AU - Marhadour, Sophie

AU - Tomasoni, Christophe

AU - Evenou, Pierre

AU - Piessard, Sylvie

AU - Vaisberg, Abraham J.

AU - Ruchaud, Sandrine

AU - Bach, Stéphane

AU - Roussakis, Christos

AU - Marchand, Pascal

PY - 2016/4

Y1 - 2016/4

N2 - 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.

AB - 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.

KW - Antiproliferative activity

KW - Imidazo[1,2-A]pyrazine

KW - NSCLC

KW - P53

KW - Urea

UR - https://www.scopus.com/pages/publications/84984533425

M3 - Artículo

C2 - 27069139

AN - SCOPUS:84984533425

SN - 0250-7005

VL - 36

SP - 1621

EP - 1630

JO - Anticancer Research

JF - Anticancer Research

IS - 4

ER -

Discovery of novel (imidazo[1,2-a]pyrazin-6-yl)ureas as antiproliferative agents targeting p53 in non-small cell lung cancer cell lines

Abstract

UN SDGs

Keywords

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