Isatin derivatives with activity against apoptosis-resistant cancer cells

Bioorg Med Chem Lett. 2016 Mar 15;26(6):1558-1560. doi: 10.1016/j.bmcl.2016.02.015. Epub 2016 Feb 8.

Abstract

In a search of small molecules active against apoptosis-resistant cancer cells, a series of isatin-based heterocyclic compounds were synthesized and found to inhibit proliferation of cancer cell lines resistant to apoptosis. The synthesis of these compounds involved a condensation of commercially available, active methylene heterocycles with isatin proceeding in moderate to excellent yields. The heterocyclic scaffolds prepared in the current investigation appear to be a useful starting point for the development of agents to fight cancers with apoptosis resistance, and thus, associated with dismal prognoses.

Keywords: Anticancer activity; Apoptosis resistance; Cytotoxic compounds; Indirubin; Isatin.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Isatin / analogs & derivatives*
  • Isatin / chemical synthesis
  • Isatin / chemistry
  • Isatin / pharmacology*
  • Molecular Structure
  • Neoplasms / pathology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Isatin