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Synthesis of stereochemically diverse cyclic analogs of tubulysins
- Issue Date
- Nov-2015
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Tubulysin; Antitumor agents; Peptides; Asymmetric catalysis; Hetero Diels-Alder reaction
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.23, no.21, pp 6827 - 6843
- Pages
- 17
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 23
- Number
- 21
- Start Page
- 6827
- End Page
- 6843
- ISSN
- 0968-0896
1464-3391
- Abstract
- 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. (C) 2015 Elsevier Ltd. All rights reserved.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)