Synthesis of stereochemically diverse cyclic analogs of tubulysins
- 주제(키워드) Antitumor agents , Asymmetric catalysis , Hetero Diels-Alder reaction , Peptides , Tubulysin
- 등재 SCIE, SCOPUS
- 발행기관 Elsevier Ltd
- 발행년도 2015
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000120200
- 본문언어 영어
- Published As http://dx.doi.org/10.1016/j.bmc.2015.10.003
- 저작권 이화여자대학교 논문은 저작권에 의해 보호받습니다.
초록/요약
The synthesis of tubulysin analogs containing stereochemically diverse cyclic Tuv moieties is described. A tetrahydropyranyl moiety was incorporated into the Tuv unit by enantioselective hetero Diels-Alder reactions of Danishefsky's diene and thiazole aldehyde. Four different stereoisomers of cyclic Tuv units were used as surrogates for the Tuv moiety. The synthesized stereochemically diverse simplified cyclic analogs were evaluated for the inhibition of tubulin polymerization. © 2015 Elsevier Ltd. All rights reserved.
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