Synthesis of a Cyclic Analogue of Tuv N-Methyl Tubulysin
- Synthesis of a Cyclic Analogue of Tuv N-Methyl Tubulysin
- 박윤정; 이재균; 유재상
- antitumor agents; peptides; Diels?Alder reaction; asymmetric
- Issue Date
- VOL 26, NO 8, 1063-1068
- Tubulysins are the most potent antimitotic agents known so far. We are interested in the conformational effect of tubulysin and herein we report the design and synthesis of a conformationally rigid cyclic analogue of Tuv N-methyl tubulysin. A conformationally rigid tetrahydropyran moiety was incorporated into the Tuv fragment via enantioselective hetero Diels-Alder reaction to prevent the rotation of the Tuv chain. The following diastereoselective reductive amination yielded the (4-methylamino)tetrahydropyranyl Tuv fragment, which was coupled to d-Mep-l-Ile dipeptide fragment and Tup fragment sequentially.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.