Abstract: OBJECTIVE To introduce the structure activity relationships (SAR) of taxanes toward multi-drug resistant tumors and progress on its clinical research. METHODS According to the correlative reports in recent years, both the modifications of taxanes and advances in the development of taxane candidates that either have potential for, or are already in, clinical use are reviewed. RESULTS A number of taxanes exhibiting virtually no difference in potency against the drug-sensitive and drug-resistant cell lines were discovered. CONCLUSION It is essential to grasp the SAR of taxanes against drug-resistant tumors and there is far-reaching significance for the discovery of new generation taxane anticancer agents.