Synthesis and in Vitro cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones

Arch Pharm Res. 2010 May;33(5):663-7. doi: 10.1007/s12272-010-0503-z. Epub 2010 May 29.

Abstract

A series of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones (4a-f) was synthesized and their in vitro cytotoxic activities were evaluated against six human cancer cell lines (HCT15, SK-OV-3, SNB19, A549, MCF7 and MCF7/ADR). They all appeared to be less potent than doxorubicin against all doxorubicin sensitive human cancer cell lines tested. However, these compounds retained considerable cytotoxic activity against the doxorubicin-resistant cell line MCF7/ADR, implying their therapeutic potential to treat doxorubicin-resistant tumors. The most active compound 4c was equipotent with doxorubicin against HCT15 cell line.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anthracenes / chemical synthesis*
  • Anthracenes / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects*
  • Doxorubicin / pharmacology
  • Drug Resistance, Neoplasm / drug effects
  • Drug Screening Assays, Antitumor / methods
  • Humans
  • Molecular Structure
  • Quantitative Structure-Activity Relationship

Substances

  • Anthracenes
  • Antineoplastic Agents
  • Doxorubicin