Five new taxane diterpenoids, taxumairols G (1), H (2), I (3), J (4), and L (5) were isolated from extracts of the roots of Taiwanese Taxus mairei (LEMEE & LEVL.) S. Y. Hu. Compounds 1-4 belong to the new 11(15-->1)-abeo-taxene system, having a tetrahydrofuran ring along carbons C-2, C-3, C-4 and C-20. Compounds 3 and 4 contain an isopropenyl group at C-1 while compounds 1 and 2 are attached wi...

The taxanes docetaxel (Taxotere; Aventis Pharmaceuticals Inc., Bridgewater, NJ, http://www.aventispharma-us.com) and paclitaxel (Taxol; Bristol-Myers Squibb, Princeton, NJ, http://www.bms.com) have significant clinical activity in metastatic breast cancer. A number of clinical trials have evaluated the tolerability and efficacy of weekly taxane administration to optimize the benefit-to-risk rat...

Microtubule-stabilizing agents (MSAs) are efficacious chemotherapeutic drugs widely used for the treatment of cancer. Despite the importance of MSAs for medical applications and basic research, their molecular mechanisms of action on tubulin and microtubules remain elusive. We determined high-resolution crystal structures of αβ-tubulin in complex with two unrelated MSAs, zampanolide and epothil...

Docetaxel remains a cornerstone of therapy for the patient with metastatic castration-resistant prostate cancer (CRPC). However, the landscape of CRPC therapy is changing rapidly - recently, data from the phase III TROPIC study revealed a survival advantage with the novel taxane cabazitaxel/prednisone (compared with mitoxantrone/prednisone) in a cohort of 755 men with docetaxel-refractory metas...

Taxanes, such as, e.g., taxinin Β 1 or taxol 2, are unu­ sual hydroxylated diterpenes which occur in plants of the family Taxaceae, to which the yew tree (Taxus baccata L.) belongs. The antileukemic and antitumoral activities of some taxanes and the problems encountered in the syn­ thesis of the unusual tricyclic carbon skeleton 3 have aroused increasing interest in recent years . According to ...