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Highly Active Ansamitocin Derivatives: Mutasynthesis Using an AHBA‐Blocked Mutant
Author(s) -
Taft Florian,
Brünjes Marco,
Floss Heinz G.,
Czempinski Nadine,
Grond Stephanie,
Sasse Florenz,
Kirschning Andreas
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700742
Subject(s) - semisynthesis , mutant , stereochemistry , chemistry , biology , biochemistry , gene
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.