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.
Aberle
Nicholas
N
The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Vic. 3050, Australia. aberle@wehi.edu.au <aberle@wehi.edu.au>
Catimel
Jenny
J
Nice
Edouard C
EC
Watson
Keith G
KG
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D011161:Porifera; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D013844:Thiazoles; C114816:naamidine A