10 Nov 2003·Angewandte Chemie International EditionQ1 · CHEMISTRY
Total Synthesis and Reassessment of the Phosphatase‐Inhibitory Activity of the Antitumor Agent TMC‐69‐6H
Q1 · CHEMISTRY
Article
Author: Alois Fürstner ; Heino Prinz ; Fabian Feyen ; Herbert Waldmann
The unexpected selectivity profile of (17R)- and (17S)-TMC-69-6H suggests that N-hydroxypyridone derivatives constitute a promising new lead structure in the search for selective phosphatase inhibitors.An unprecedented Pd-catalyzed C-C bond formation to a pyranone derivative to form I was a key step in the synthesis of enantiopure (17R)- (II) and (17S)-TMC-69-6H.
01 Jan 2001·The Journal of AntibioticsQ4 · MEDICINE
TMC-69, a New Antitumor Antibiotic with Cdc25A Inhibitory Activity, Produced by Chrysosporium sp. TC1068.
A new antibiotic designated TMC-69 has been isolated from the fermentation broth of a fungal strain Chrysosporium sp. TC 1068. TMC-69 exhibited moderate in vitro cytotoxic activity. TMC-69-6H, a derivative of TMC-69 prepared by hydrogenation, possessed more potent in vitro cytotoxicity than TMC-69, and exhibited in vivo antitumor activity against murine P388 leukemia and B16 melanoma. TMC-69-6H was found to specifically inhibit Cdc25A and B phosphatases.
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