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

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.

• Authors: Igor V Magedov, Florence Lefranc, Liliya V Frolova, Laetitia Moreno Y Banuls, Amanda S Peretti, Snezna Rogelj, Véronique Mathieu, Robert Kiss, Alexander Kornienko
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 11 Pg. 3277-82 (Jun 01 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 23622980 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Indoles

Topics

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