By utilizing an l-serine-derived bicyclic lactone as an advanced chiral building block, a short synthetic route to the cytotoxic marine natural product jaspine B has been developed. Targeting structure-activity relationship investigations, the synthetic route has also been utilized for the synthesis and cytotoxicity evaluation of strategically modified jaspine B analogues. In addition, a previously reported synthesis of the title natural product from our research has been reinvestigated to clarify the sterochemical assignment.
Bibliographical notePublisher Copyright:
© Georg Thieme Verlag Stuttgart · New York-Synthesis 2017.
- drug development
- jaspine B
- structure-activity relationships