Drug-initiated, controlled ring-opening polymerization for the synthesis of polymer-drug conjugates
Paclitaxel, a polyol chemotherapeutic agent, was covalently conjugated through its 2′-OH to polylactide with 100% regioselectivity via controlled polymerization of lactide mediated by paclitaxel/(BDI-II)ZnN(TMS)2 (BDI-II = 2-((2,6-diisopropylph
Tong, Rong,Cheng, Jianjun
experimental part
p. 2225 - 2232
(2012/06/18)
Synthesis of congeners and prodrugs. 3. Water-soluble prodrugs of taxol with potent antitumor activity
Taxol has shown good in vivo antitumor activity in a number of test systems. The formulation of taxol for antitumor testing has been difficult. Esterification at either C-2' or C-7 resulted in loss of in vitro tubulin assembly activity but not cytotoxicit