Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines

Exp Oncol. 2008 Jun;30(2):139-42.

Abstract

Quinazolines are known to be multitarget agents with broad spectrum of biological activity.

Aim: To investigate anticancer activity of newly prepared 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline (BMAQ) towards L1210, HL-60 and U-937 leukemia cells.

Materials and methods: Growth inhibition of BMAQ-treated cells was determined by cell counting using trypan blue staining technique. Apoptosis and cell cycle profile changes were analysed using internucleosomal DNA fragmentation assay, fluorescence microscopy and flow cytometry. Activity of caspase-3 was determined using colorimetric method.

Results: Cell proliferation assay showed that BMAQ caused significant decrease of cell number in a dose-dependent manner. BMAQ induced cell death by apoptosis, based on results from DNA fragmentation, fluorescence microscopy and caspase-3 assays.

Conclusion: Presented results clearly demonstrate that BMAQ is a promising anticancer agent with significant antiproliferative and apoptotic activities towards leukemia cells in vitro.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / pharmacology*
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Apoptosis*
  • Cell Line, Tumor
  • Cell Proliferation
  • DNA Fragmentation
  • Drug Screening Assays, Antitumor
  • HL-60 Cells
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Microscopy, Fluorescence
  • Models, Chemical
  • Quinazolines / pharmacology*
  • U937 Cells

Substances

  • 6-hydroxypropynyl-4-anilinoquinazoline
  • Aniline Compounds
  • Antineoplastic Agents
  • Quinazolines