Tubulysins are strongly cytotoxic natural tetrapeptides with potent anti-proliferative, anti-mitotic and anti-angiogenic activities which might find use in oncology. We herein report the first total synthesis of a stereoisomerically pure oxazole analogue of tubulysin U, which was found to be more cytotoxic than the thiazole-containing natural product. Additionally, we have developed an improved and scalable synthetic route towards the Tup fragment of the tubulysins.
- SAR study
Shankar, P. S., Sani, M., Zanda, M., Saunders, F., & Wallace, H. M. (2011). Total synthesis and cytotoxicity evaluation of an oxazole analogue of tubulysin U. Synlett, 12(12), 1673-1676. https://doi.org/10.1055/s-0030-1260806