Discovery of Novel (Imidazo[1,2-a]pyrazin-6-yl)ureas as Antiproliferative Agents Targeting P53 in Non-small Cell Lung Cancer Cell Lines

作者：Bazin Marc Antoine; Rousseau Benedicte; Marhadour Sophie; Tomasoni Christophe; Evenou Pierre; Piessard Sylvie; Vai**erg Abraham J; Ruchaud Sandrine; Bach Stephane; Roussakis Christos; Marchand Pascal

来源：Anticancer Research, 2016, 36(4): 1621-1630.

• Imidazo[1,2-a]pyrazine
• urea
• antiproliferative activity
• NSCLC
• p53

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.

• 出版日期2016-4