Scaffold hybridization in generation of indenoindolones as anticancer agents that induce apoptosis with cell cycle arrest at G2/M phase

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2474-9. doi: 10.1016/j.bmcl.2012.02.007. Epub 2012 Feb 11.

Abstract

Scaffold hybridization of several natural and synthetic anticancer leads led to the consideration of indenoindolones as potential novel anticancer agents. A series of these compounds were prepared by a diversity-feasible synthetic method. They were found to possess anticancer activities with higher potency compared to etoposide and 5-fluorouracil in kidney cancer cells (HEK 293) and low toxicity to corresponding normal cells (Vero). They exerted apoptotic effect with blocking of cell cycle at G2/M phase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects*
  • Biomarkers / metabolism
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Etoposide / pharmacology
  • Flow Cytometry
  • Fluorouracil / pharmacology
  • G2 Phase Cell Cycle Checkpoints / drug effects*
  • HEK293 Cells
  • Humans
  • Indenes / chemical synthesis*
  • Indenes / pharmacology
  • Indoles / chemical synthesis*
  • Indoles / pharmacology
  • Inhibitory Concentration 50
  • Vero Cells

Substances

  • Antineoplastic Agents
  • Biomarkers
  • Indenes
  • Indoles
  • Etoposide
  • Fluorouracil