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Precursor-directed generation of amidine containing ammosamide analogs: Ammosamides E-P

Ende Pan; Nathaniel W. Oswald; Aaron G. Legako; Janie M. Life; Bruce A. Posner; John B. MacMillan

(Profiled Authors: John B MacMillan; Bruce A Posner)

Chemical Science. 2013;4(1):482-488.


Ammosamides E-F (1-2), are amidine analogs of the ammosamide family of alkaloids isolated from a marine-derived Streptomyces variabilis. Further studies with S. variabilis revealed a variety of aryl and alkyl amines added into the fermentation media could be efficiently incorporated into the ammosamide framework to generate a library of precursor-directed amidine analogs, ammosamides G-P (9-18). We demonstrate that the amines are introduced via non-enzymatic addition to the iminium ion of ammosamide C. Biological evaluation of the amidine analogs against quinone reductase 2 (QR2) showed low nM potency for a number of analogs. When tested for in vivo activity against a panel of non-small cell lung cancer (NSCLC) cell-lines there was a clear increase in potency by incorporation of lipophilic alkylamines, with the most potent compounds having sub μM IC50 values (0.4 to 0.8 μM). © 2013 The Royal Society of Chemistry.

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