Total synthesis and cytotoxicity evaluation of an oxazole analogue of tubulysin U

P.S. Shankar, M. Sani, Matteo Zanda, Fiona Saunders, H.M. Wallace

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

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.
Original languageEnglish
Pages (from-to)1673-1676
Number of pages4
JournalSynlett
Volume12
Issue number12
DOIs
Publication statusPublished - 1 Jan 2011

Keywords

  • tubulysin
  • oxazole
  • SAR study
  • chemotherapy
  • cytotoxicity

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