Synthesis and biological evaluation of analogues of the anti-tumor alkaloid naamidine A.

Abstract

A small series of derivatives of the alkaloid naamidine A was synthesized and tested in vitro for their ability to inhibit mitogenesis in BaF/ERX cells. Replacement of the imidazole core with a thiazole was found to have only a minor effect on potency, and the 4-methoxybenzyl substituent of the natural product was shown to be unnecessary for activity.

• Authors: Nicholas Aberle, Jenny Catimel, Edouard C Nice, Keith G Watson
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 13 Pg. 3741-4 (Jul 01 2007) ISSN: 0960-894X [Print] England
• PMID: 17462892 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Enzyme Inhibitors
• Imidazoles
• Thiazoles
• naamidine A

Topics

• Animals
• Antineoplastic Agents (pharmacology)
• Cell Line
• Chemistry, Pharmaceutical (methods)
• Drug Design
• Drug Screening Assays, Antitumor
• Enzyme Inhibitors (chemistry, pharmacology)
• Imidazoles (chemical synthesis, chemistry, pharmacology)
• Inhibitory Concentration 50
• Mice
• Models, Chemical
• Porifera
• Structure-Activity Relationship
• Thiazoles (chemistry)