Development of 3-aryl-1-isoquinolinamines as potent antitumor agents based on CoMFA

Eur J Med Chem. 2010 Nov;45(11):5493-7. doi: 10.1016/j.ejmech.2010.08.042. Epub 2010 Aug 24.


Various substituted 3-aryl-1-isoquinolinamines were designed and synthesized based on the previously constructed CoMFA model. Most of the synthesized compounds showed excellent potency in eight different human tumor cell lines as expected. In order to find the exact cytotoxic mechanism of these 3-aryl-1-isoquinolinamines, we analyzed the cell cycle dynamics by flow cytometry and found that 3-aryl-1-isoquinolinamine 6k-treated HeLa cells were arrested in G2/M phase, which is related to apoptosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry*
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Flow Cytometry
  • Humans
  • Isoquinolines / chemistry*
  • Isoquinolines / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry


  • Amines
  • Antineoplastic Agents
  • Isoquinolines