PUB - Publikationen an der Universität Bielefeld

Many of today's most efficient anticancer chemotherapeutics interfere with microtubule dynamics. They prevent microtubules from forming correct mitotic spindles, therefore cause an arrest of the cell-division cycle and eventually trigger programmed cell death (apoptosis). Prominent examples of these type of drugs are the Vinca alkaloids, taxanes, and epothilones. Among newly discovered agents with a microtubule-destabilizing mechanism of action, the cryptophycins are highly promising drug candidates, since their biological activity is not negatively affected by P-glycoprotein, a drug efflux system commonly found in multiply drug resistant cancer cell lines. This short account is intended to outline the currently known biological activity profile of cryptophycins, as well as the state of the art in cryptophycin synthesis. Focus is placed on the most recent and successful strategies to assemble the structurally challenging unit A and its benzylic epoxide function.