Microbial Transformation of Trichostatin A to 2,3-Dihydrotrichostatin A
摘要:
A new reduced hydroxamate, 2,3-dihydrotrichostatin A, was created from trichostatin A by employing a recombinant strain of Streptomyces venezuelae as a microbial catalyst. Compared with trichostatin A, 2,3-dihydrotrichostatin A showed similar antifungal activity against Saccharomyces cerevisiae, but, interestingly, approximately twice the cytostatic activity against human small cell lung cancer cells. The production of 2,3-dihydrotrichostatin A via microbial biotransformation demonstrates that the regiospecific and substrate-flexible hydrogenation by S. venezuelae provides a new approach for creating natural product analogues with improved bioactive properties.
申请人:GlaxoSmithKline Intellectual Property Development Limited
公开号:US20200299309A1
公开(公告)日:2020-09-24
The invention relates a compound of the formula:
a pharmaceutically acceptable salt thereof, compositions thereof, and methods of therapeutic treatment using the same.