Tunable Thioesters as “Reduction” Responsive Functionality for Traceless Reversible Protein PEGylation
摘要:
Disulfide has been the only widely used functionality to serve as a reduction responsive trigger in drug delivery. We introduce thioester as a novel thiol responsive chemistry for drug delivery, whose reactivity can be conveniently modulated by choosing the appropriate steric environment around the thioester. Compared with disulfides, thioesters are facile to synthesize and have an order of magnitude broader kinetic tunability. A novel traceless reversible protein PEGylation reagent is developed based on thioester chemistry.
The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are also disclosed.
本发明涉及长春花生物碱衍生物。还公开了包含这些化合物的药物组合物以及制备和治疗各种疾病的过程。
VINCA DERIVATIVES
申请人:SCOTT L. Ian
公开号:US20080108644A1
公开(公告)日:2008-05-08
The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are also disclosed.