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New, Highly Active Nonbenzoquinone Geldanamycin Derivatives by Using Mutasynthesis
Author(s) -
Eichner Simone,
Floss Heinz G.,
Sasse Florenz,
Kirschning Andreas
Publication year - 2009
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.200900246
Subject(s) - geldanamycin , hsp90 , natural product , chemistry , stereochemistry , streptomyces hygroscopicus , mutant , semisynthesis , biochemistry , heat shock protein , biology , streptomyces , gene , genetics , bacteria
You are what you eat : The feeding of aromatic and heteroaromatic amino acids to an AHBA‐blocked mutant of S. hygroscopicus yielded new analogues of the highly potent Hsp90 inhibitor geldanamycin. Except for a “pyridine”‐geldanamycin derivative, all new compounds had strong antiproliferative activity (IC 50 values in the n M range).