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Total Synthesis of Tubulysin U and V

✍ Scribed by Alexander Dömling; Barbara Beck; Uwe Eichelberger; Sukumar Sakamuri; Sanjay Menon; Quin-Zene Chen; Yingchun Lu; Ludger A. Wessjohann

Publisher
John Wiley and Sons
Year
2006
Tongue
English
Weight
125 KB
Volume
45
Category
Article
ISSN
0044-8249

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✦ Synopsis

Tubulysins (1) are compounds of extraordinary potency, rapidly degrading the tubulin cytoskeleton, with tubulysin D being the most active tubulin-modifier known so far. [1,2] The tubulysins were first described by Höfle, Reichenbach, and co-workers in 2000. [3,4] Several representatives are active with GI 50 values (growth inhibition of 50 %) in the low picomolar range against the NCI-60 cancer cell-line panel, and some are highly antiangiogenic. [5] Semisynthetic tubulysins, derived from isolated material, show promising in vivo anticancer properties and are candidates for antibody conjugates. Thus, tubulysins are attractive leads as novel anticancer agents. [5] However, so far, tubulysins can only be produced by a fermentation process that yields less than 10 mg L À1 by several rather tedious chromatographic purification steps. Thus, and

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Total Synthesis of Tubulysin U and V
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✍ Alexander Dömling; Barbara Beck; Uwe Eichelberger; Sukumar Sakamuri; Sanjay Meno 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 English ⚖ 62 KB 👁 1 views
Total Synthesis of Tubulysin U and V
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