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

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

doi:10.1055/s-0030-1260806

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 journal › Article › peer-review

17 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 language	English
Pages (from-to)	1673-1676
Number of pages	4
Journal	Synlett
Volume	12
Issue number	12
DOIs	https://doi.org/10.1055/s-0030-1260806
Publication status	Published - 1 Jan 2011

Keywords

tubulysin
oxazole
SAR study
chemotherapy
cytotoxicity

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10.1055/s-0030-1260806

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AU - Sani, M.

AU - Zanda, Matteo

AU - Saunders, Fiona

AU - Wallace, H.M.

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KW - oxazole

KW - SAR study

KW - chemotherapy

KW - cytotoxicity

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ER -

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

Abstract

Keywords

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