Oligolactic acid conjugates and micelles with improved anticancer efficacy

摘要

The present invention generally relates to oligolactic acid conjugates of paclitaxel, rapamycin, cellomethinib and other anticancer agents, a micelle composition containing the conjugates, and methods of treating various cancers by making and using the compositions. Specifically, it is preferred that the oligolactic acid comprises 2 to 24 lactic acid subunits and the 40-hydroxyl of the 7-hydroxyl, rapamycin or rapamycin derivative of the paclitaxel or paclitaxel derivative, and the 2 ' of the cellomethinib or & An oligolactic acid conjugate conjugated via ester linkage to oxygen in the hydroxyl is provided. water; And a composition comprising a polylactic acid-containing polymer and a micelle comprising an oligolactic acid conjugate can be easily prepared. Also provided is a method of inhibiting or killing cancer cells and treating paclitaxel, rapamycin and / or cellometinib cancer.