Synthesis of 9-acridinyl sulfur derivatives: sulfides, sulfoxides and sulfones. Comparison of their activity on tumour cells

The synthesis of several acridine thioethers is described. These compounds were oxidized to give new sulfoxides and sulfones. Among 23 compounds prepared, 19 were tested in vitro against the human cancer cell lines panel of NCI screening. Activity is increased 5–10 times from sulfides to sulfoxides....

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Veröffentlicht in:	European journal of medicinal chemistry 2004-12, Vol.39 (12), p.1029-1038
Hauptverfasser:	Santelli-Rouvier, Christiane, Barret, Jean-Marc, Farrell, Christopher M., Sharples, Derek, Hill, Bridget T., Barbe, Jacques
Format:	Artikel
Sprache:	eng
Schlagworte:	Acridine sulfides Anticancer activity Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects DNA Damage - drug effects DNA interaction Drug Screening Assays, Antitumor General aspects Humans Medical sciences Molecular Structure Pharmacology. Drug treatments Saccharomyces cerevisiae - drug effects Structure-Activity Relationship Sulfides - chemical synthesis Sulfides - pharmacology Sulfones Sulfones - chemical synthesis Sulfones - pharmacology Sulfoxides Sulfoxides - chemical synthesis Sulfoxides - pharmacology
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Zusammenfassung:	The synthesis of several acridine thioethers is described. These compounds were oxidized to give new sulfoxides and sulfones. Among 23 compounds prepared, 19 were tested in vitro against the human cancer cell lines panel of NCI screening. Activity is increased 5–10 times from sulfides to sulfoxides. Among substituted groups in the side chain, sulfur mustard, epoxy sulfide and sulfoxide displayed the most interesting activity.
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2004.06.015