Design, synthesis and biological evaluation of substituted 11H-benzo[a]carbazole-5-carboxamides as novel antitumor agents

Eur J Med Chem. 2011 Dec;46(12):5878-84. doi: 10.1016/j.ejmech.2011.09.050. Epub 2011 Oct 4.

Abstract

A series of novel 11H-benzo[a]carbazole-5-carboxamide derivatives were designed, synthesized and evaluated for their antitumor activity against human cancer A549 and HCT-116 cell lines. Most of the compounds showed potent antitumor activities, and compound 8 displayed remarkable in vitro and in vivo anticancer activity comparable to that of amonafide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry
  • Amides / pharmacology
  • Amides / therapeutic use
  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Carbazoles / chemical synthesis
  • Carbazoles / chemistry*
  • Carbazoles / pharmacology
  • Carbazoles / therapeutic use*
  • Cell Cycle Checkpoints / drug effects
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Mice
  • Mice, Nude
  • Neoplasms / drug therapy
  • Structure-Activity Relationship

Substances

  • Amides
  • Antineoplastic Agents
  • Carbazoles
  • carbazole