Anti-tumor effects of B-2, a novel 2,3-disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazoline derivative, on the human lung adenocarcinoma A549 cell line in vitro and in vivo

作者：Chen, Zhe; Huang, Xin; Yang, Hongyu; Ding, Wenbo; Gao, Lingyan; Yea, Ziqi; Zhang, Yandong; Yu, Yongping^*; Lou, Yijia

来源：Chemico-Biological Interactions, 2011, 189(1-2): 90-99.

DOI：10.1016/j.cbi.2010.11.004

• Quinazoline derivative
• A549 cell line
• Transplant tumor
• G1 arrest
• Apoptosis

This study evaluated the selective effects of 2-isopropyl-3-butyl-8-(4-fluorophenylamino)-3H-imidazo[4,5-g]quinazoline (B-2), a member of a series of quinazolines, on the cell survival and growth of the non-small cell lung cancer (NSCLC) cell line A549 in vitro and in vivo. Cytotoxicity assay, hollow fiber assay and cell xenograft model experiment revealed that B-2 showed selective effects on A549 cell survival or growth in a dose-dependent manner. At a dose of 100 mg/kg, B-2 showed stronger efficacy on tumor growth inhibition in nude mice than lressa. Exposure of A549 cells to B-2 caused inhibition of EGFR-dependent ERK-MAPK activation. In addition, inhibition of cell cycle progression and induction of mitochondria-dependent apoptosis might contribute to present the multitarget pathway of non-small cell lung cancer treatment of B-2.

• 出版日期2011-1-15
• 单位浙江大学