Investigating the antiproliferative activity of quinoline-5,8-diones and styrylquinolinecarboxylic acids on tumor cell lines.

Abstract

The structure-activity relationships of new quinoline based compounds were investigated. Quinoline-5,8-dione and styrylquinoline scaffolds were used for the design of potentially active compounds. The novel analogues had comparable antiproliferative activity to cisplatin when evaluated in a bioassay against the P388 leukemia cell line. However, these compounds appeared far less efficient against SK-N-MC neuroepithelioma cells. Analogues without the 5,8-dione structure but containing the 8-carboxylic acid group were also found to induce antiproliferative activity. Hydrophobicity as measured by HPLC did not correlate with antiproliferative activity.

• Authors: B Podeszwa, H Niedbala, J Polanski, R Musiol, D Tabak, J Finster, K Serafin, M Milczarek, J Wietrzyk, S Boryczka, W Mol, J Jampilek, J Dohnal, D S Kalinowski, D R Richardson
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 22 Pg. 6138-41 (Nov 15 2007) ISSN: 0960-894X [Print] England
• PMID: 17904844 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Carboxylic Acids
• Quinolines
• styrylquinoline

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Carboxylic Acids (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Drug Screening Assays, Antitumor
• Humans
• Mice
• Molecular Structure
• Quinolines (chemical synthesis, chemistry, pharmacology)
• Structure-Activity Relationship