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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.

Abstract
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 100mg/kg, B-2 showed stronger efficacy on tumor growth inhibition in nude mice than Iressa. 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.
AuthorsZhe Chen, Xin Huang, Hongyu Yang, Wenbo Ding, Lingyan Gao, Ziqi Ye, Yandong Zhang, Yongping Yu, Yijia Lou
JournalChemico-biological interactions (Chem Biol Interact) Vol. 189 Issue 1-2 Pg. 90-9 (Jan 15 2011) ISSN: 1872-7786 [Electronic] Ireland
PMID21075094 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2010 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Imidazoles
  • Quinazolines
  • EGFR protein, human
  • ErbB Receptors
  • Mitogen-Activated Protein Kinases
Topics
  • Animals
  • Antineoplastic Agents (pharmacology)
  • Carcinoma, Non-Small-Cell Lung (drug therapy, metabolism, pathology)
  • Cell Cycle (physiology)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • ErbB Receptors (antagonists & inhibitors, metabolism)
  • Flow Cytometry
  • Humans
  • Imidazoles (pharmacology)
  • Lung Neoplasms (drug therapy, metabolism, pathology)
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Microscopy, Confocal
  • Mitogen-Activated Protein Kinases (antagonists & inhibitors, metabolism)
  • Molecular Dynamics Simulation
  • Phosphorylation (drug effects)
  • Quinazolines (pharmacology)
  • Xenograft Model Antitumor Assays

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