Abstract

Structure activity relationship (SAR) and mechanism of paclitaxel and its analogues in recent years are discussed in the following areas: SAR of paclitaxel analogues toward “normal” and multi-drug resistance tumors; paclitaxel prodrugs with improved water solubitily and specificity; mechanism of paclitaxel related to tubulin binding and quest for its pharmacophore.

Keywords: anticancer drugs, paclitaxel, structure-activity relationship (sar), multi-drug resistance (mdr), prodrugs, microtubule, pharmacophore