Antiproliferative activity of 2,3-disubstituted indoles toward apoptosis-resistant cancers cells

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3277-82. doi: 10.1016/j.bmcl.2013.03.110. Epub 2013 Apr 8.

Abstract

Many types of cancer, including glioma, melanoma, NSCLC, among others, are resistant to apoptosis induction and poorly responsive to current therapies with propaptotic agents. We describe a series of 2,3-disubstituted indoles, which display cytostatic rather than cytotoxic effects in cancer cells, and serve as a new chemical scaffold to develop anticancer agents capable of combating apoptosis-resistant cancers associated with dismal prognoses.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / toxicity
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry*
  • Indoles / toxicity
  • Mice
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Indoles