Molekül des Monats
1st September 2014
First isolated in 1972 from the African plant Maytenus ovatus, later named Maytenus serrata, by Professor S. Morris Kupchan and co-workers at the University of Virginia using bioassay-guided methods, the 19-membered macrolactam maytansine (CHEBI:6701) was found to combine broad spectrum antitumour activity with extraordinarily high potency . However, it took a further five years before a more efficient isolation procedure was developed using M. buchananii and sufficient quantities of maytansine became available to enable clinical trials to proceed. In the meantime, with funding particularly from the US National Cancer Institute, a number of closely related compounds known as 'maytansinoids' were isolated from members of the bittersweet (Celastraceae), buckthorn (Rhamnaceae), and spurge (Euphorbiaceae) plant families. Unfortunately, early hopes that maytansine or maytansinoids could be readily developed into a clinically useful anticancer drug were dashed by disappointing Phase II clinical trials, probably a result of the dose-limiting cytotoxicity of the maytansinoids in humans.Read more ...