Synthesis and Biological Evaluation of New Bis-Indolinone Derivatives Endowed with Cytotoxic Activity.

Abstract

A series of new Knoevenagel adducts, bearing two indolinone systems, has been synthesized and evaluated on 60 human cancer cell lines according to protocols available at the National Cancer Institute (Bethesda, MD, USA). Some derivatives proved to be potent antiproliferative agents, showing GI50 values in the submicromolar range. Compound 5b emerged as the most active and was further studied in Jurkat cells in order to determine the effects on cell-cycle phases and the kind of cell death induced. Finally, oxidative stress and DNA damage induced by compound 5b were also analyzed.

• Authors: Rita Morigi, Elena Catanzaro, Alessandra Locatelli, Cinzia Calcabrini, Valentina Pellicioni, Alberto Leoni, Carmela Fimognari
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 26 Issue 20 (Oct 16 2021) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 34684858 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Oxindoles

Topics

• Antineoplastic Agents (pharmacology)
• Apoptosis (drug effects)
• Cell Cycle (drug effects)
• Cell Death (drug effects)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• DNA Damage (drug effects)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor (methods)
• Humans
• Jurkat Cells
• Molecular Structure
• Oxidative Stress (drug effects)
• Oxindoles (pharmacology)