Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5722-5. doi: 10.1016/j.bmcl.2010.08.010. Epub 2010 Aug 6.

Abstract

The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC(50)=0.006 μM) and good selectivity over HS27 fibroblast cell line.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Chromones / chemical synthesis*
  • Chromones / chemistry
  • Chromones / therapeutic use
  • Humans
  • Melanoma / drug therapy
  • Quinazolines / chemical synthesis
  • Quinazolines / chemistry*
  • Quinazolines / therapeutic use
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Chromones
  • Quinazolines