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 non-small 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.

Cite this paper

@article{Bazin2016DiscoveryON, 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.}, author={M Bazin and B{\'e}n{\'e}dicte Rousseau and Sophie Marhadour and Christophe Tomasoni and Pierre {\'E}venou and Sylvie Piessard and Abraham J Vaisberg and Sandrine Ruchaud and St{\'e}phane Bach and Christos Roussakis and Pascal Marchand}, journal={Anticancer research}, year={2016}, volume={36 4}, pages={1621-30} }