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

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.

The syntheses of deletion analogues and thiazole analogues of naamidine A (1) are reported, together with data indicating inhibition of EGF- and IL3-dependent mitogenesis.Figure optionsDownload as PowerPoint slide