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.
Nikolai M Evdokimov  1 ,  Igor V Magedov  2 ,  Dominic McBrayer  2 ,  Alexander Kornienko  3
Affiliations
  • 1. Department of Molecular and Medical Pharmacology, University of California, Los Angeles, CA 90095, United States; Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States. Electronic address: [email protected].
  • 2. Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States.
  • 3. Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, United States. Electronic address: [email protected].
PMID: 26883150 DOI: 10.1016/j.bmcl.2016.02.015
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.