Article
Assessing oxazole bioisosteres as mutasynthons on the rhizoxin assembly line.
Chembiochem : a European journal of chemical biology - 17 Oct 2011
Kusebauch Björn, Brendel Nicole, Kirchner Heike, Dahse Hans-Martin, Hertweck Christian
Abstract excerpt
Chain armor against tumor cells: The oxazole side chain in the antimitotic agent rhizoxin S2 (1) was successfully replaced through mutasynthesis by using an engineered mutant impaired in heterocyclization. Incorporation of 12 non-natural surrogates into fully processed rhizoxin analogues revealed a remarkable substrate flexibility of the PKS-NRPS hybrid.
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