Highly Active Ansamitocin Derivatives: Mutasynthesis Using an AHBA-Blocked Mutant

Highly Active Ansamitocin Derivatives: Mutasynthesis Using an AHBA-Blocked Mutant

Feeding of halogenated 3‐aminobenzoic acids to an AHBA‐blocked mutant of Actinosynnema pretiosum (HGF073) yielded new analogues of the highly potent antitumor agent ansamitocin P‐3 (AP‐3). Combined mutasynthesis–semisynthesis was carried out by Pd‐catalyzed vinylation under Stille conditions. The ne...

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Veröffentlicht in:Chembiochem : a European journal of chemical biology 2008-05, Vol.9 (7), p.1057-1060
Hauptverfasser: Taft, Florian, Brünjes, Marco, Floss, Heinz G, Czempinski, Nadine, Grond, Stephanie, Sasse, Florenz, Kirschning, Andreas
Format: Artikel
Sprache:eng
Schlagworte:
Actinomycetales - genetics
Actinomycetales - metabolism
Aminobenzoates - metabolism
ansamitocin
antitumor agents
Hydroxybenzoates
Maytansine - analogs & derivatives
Maytansine - biosynthesis
Maytansine - chemistry
Maytansine - metabolism
mutasynthesis
Mutation
semisynthesis
Stille reaction
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Zusammenfassung:Feeding of halogenated 3‐aminobenzoic acids to an AHBA‐blocked mutant of Actinosynnema pretiosum (HGF073) yielded new analogues of the highly potent antitumor agent ansamitocin P‐3 (AP‐3). Combined mutasynthesis–semisynthesis was carried out by Pd‐catalyzed vinylation under Stille conditions. The new AP‐3 derivatives show strong antiproliferative activity against several tumor cell lines.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.200700742