Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.
The synthesis of new "selectively activated" enediyne prodrugs is reported. These compounds, belonging to the "lactenediyne" family, each possess a protected primary amine tethered at the beta-lactam nitrogen. This, once deblocked, can act as a trigger, provoking a cascade of events probably terminating with Bergman cycloaromatization of the enediyne moiety. In vitro experiments on plasmid DNA have shown that the protected compounds are inactive, while the unprotected amine is able to provoke single-strand scissions. These results open the way towards development of enzymatically activated lactenediyne prodrugs.
Process for Preparing Cyclic Esters Comprising Unsaturated Functional groups And Polyesters Prepared From Same
申请人:Markland Peter
公开号:US20130171261A1
公开(公告)日:2013-07-04
Disclosed herein are process for preparing cyclic esters comprising unsaturated functional groups. Also disclosed are copolymers prepared from the cyclic esters. The copolymers can be used to form microparticles, polymer micelles, etc., which are useful in drug delivery applications.