Colchicine, the major alkaloid of the meadow saffron, is one of the most prominent natural products and, like other tubulin-binding natural products (e.g. taxol and the epothilones), exhibits great pharmaceutical potential. The first syntheses in the late 1950s were milestones in natural product synthesis. But even today this structurally supposedly simple molecule poses a challenge to syntheti...

Two syntheses of the C(7)–C(16)-fragment 41 of epothilone D 2 were developed that were based on tin(IV) bromide mediated reactions of 5,6-difunctionalised hex-2-enylstannanes with aldehydes. In the first synthesis, (5S)-6-tert-butyldimethylsilyloxy-5-hydroxy-2-methylhex-2-enyl(tributyl)stannane 20 was reacted with (E)-but-2-enal to give (2S,7R,4Z,8E)-1-tert-butyldimethylsilyloxy-5-methyldeca-4,...

Epothilones (Epo’s) are bacterial natural products which are potent inhibitors of human cancer cell proliferation in vitro and in vivo. Tumor growth inhibition is based on the stabilization of cellular microtubules and at least seven epothilone-derived agents are presently undergoing clinical evaluation in humans. While all of these compounds are closely related structurally to the natural prod...

The taccalonolides are novel antimitotic microtubule stabilizers that have a unique mechanism of action independent of a direct interaction with tubulin. Cytotoxicity and clonogenic assays show that taccalonolide A and radiation act in an additive manner to cause cell death. The taxanes and epothilones have utility when combined with radiotherapy and these findings further suggest the additive ...

Taxol is an antitumor drug approved by the FDA for the treatment of ovarian, breast and non-small-cell lung carcinomas. Originally isolated from the bark of the Pacific yew, Taxus brevifolia, it was the first natural product described that stabilized microtubules. In the past five years, a group of novel natural products, including the epothilones, discodermolide, eleutherobin, sarcodictyins an...

Glioblastoma, the most common primary brain malignancy, is an exceptionally fatal cancer. Lack of suitable biomarkers and efficient treatment largely contribute to therapy failure. Cytoskeletal proteins are crucial in glioblastoma pathogenesis can potentially serve as therapeutic targets. Among them, GFAP, has gained attention potential diagnostic biomarker, while vimentin microtubules consider...