Author/Authors :
Mahendra D. Chordia، نويسنده , , Haiqing Yuan، نويسنده , , Prakash G. Jagtap، نويسنده , , John F. Kadow، نويسنده , , Byron H. Long، نويسنده , , Craig R Fairchild، نويسنده , , Kathy A Johnston، نويسنده , , David G.I Kingston، نويسنده ,
Abstract :
The 2,4-diacyl paclitaxel analogues 8a–8r were prepared from paclitaxel by acylation of 4-deacetyl-2-debenzoylpaclitaxel 1,2-carbonate () followed either by hydrolysis of the carbonate and acylation or by direct treatment of the carbonate with an aryllithium. Some of the resulting derivatives showed significantly improved tubulin assembly activity and cytotoxicity as compared with paclitaxel; in some cases this improvement was especially significant for paclitaxel-resistant cell lines.
