4.5 Article

Isatin derivatives with activity against apoptosis-resistant cancer cells

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 6, Pages 1558-1560

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.02.015

Keywords

Anticancer activity; Apoptosis resistance; Indirubin; Isatin; Cytotoxic compounds

Funding

  1. Phelps Family Foundation
  2. Ahmanson Translational Imaging Division, UCLA

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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. (C) 2016 Elsevier Ltd. All rights reserved.

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