Michael Best & Friedrich LLP
Deuterated dehydrophenylahistin compounds and preparation method thereof and use thereof in preparation of anti-tumor drugs
Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehydrophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.
MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD.
A C C A C C
A61P C07B C07B A61K C07D C07D
inventional inventional inventional inventional inventional inventional
Shixiao Jianchun Bing Tianwen Wenbao Huashi
Wang Zhao Cai Sun Li Guan