Preliminary SAR on indole-3-carbinol and related fragments reveals a novel anticancer lead compound against resistant glioblastoma cells

Bioorg Med Chem Lett. 2017 Apr 1;27(7):1561-1565. doi: 10.1016/j.bmcl.2017.02.033. Epub 2017 Feb 17.

Abstract

The prognosis for glioblastoma patients is, at best, poor, with the median time of survival after diagnosis measured in months. As such, there is much need for the rapid development of potent and novel treatments. Herein, we report our preliminary findings on the SAR of a series of indole-3-carbinol and related fragments and reveal a potent lead with low micromolar activity against a particularly resistant glioblastoma cell culture, providing a new platform for future development of a new therapy in this area.

Keywords: 3,3′-Diindoloylmethane; Cancer; Glioblastoma; Indole-3-carbinol; SAR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Brain Neoplasms / drug therapy*
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Glioblastoma / drug therapy*
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Indoles
  • bis(2-phenyl-1H-indol-3-yl)methane
  • indole
  • indole-3-carbinol
  • 2-phenylindole
  • 3,3'-diindolylmethane