Total synthesis of spiruchostatin A and structural analogues
Total synthesis of spiruchostatin A and structural analogues
Spiruchostatin A is a recently isolated bicyclic depsipeptide from the protobacterium Pseudomonas sp.by Shin-ya et al. It bears a resemblance to FK228, a potent inhibitor of histone deacetylase (HDACs). HDACs inhibitors are currently of great interest as anticancer agents, and examples have now advanced to phase II clinical trials. The total synthesis of spiruchostatin A and the structural analogues was accomplished. This work unambiguously confirms the structure of spiruchostatin A. Biological testing shows spiruchostatin A to be a potent HDAC inhibitor. The synthetic route is suitable for the preparation of novel spiruchostatin and FK228 analogues.
University of Southampton
Yurek-George, Alexander
bf3e1ac0-1459-4c95-93da-d7adba966f39
2004
Yurek-George, Alexander
bf3e1ac0-1459-4c95-93da-d7adba966f39
Yurek-George, Alexander
(2004)
Total synthesis of spiruchostatin A and structural analogues.
University of Southampton, Doctoral Thesis.
Record type:
Thesis
(Doctoral)
Abstract
Spiruchostatin A is a recently isolated bicyclic depsipeptide from the protobacterium Pseudomonas sp.by Shin-ya et al. It bears a resemblance to FK228, a potent inhibitor of histone deacetylase (HDACs). HDACs inhibitors are currently of great interest as anticancer agents, and examples have now advanced to phase II clinical trials. The total synthesis of spiruchostatin A and the structural analogues was accomplished. This work unambiguously confirms the structure of spiruchostatin A. Biological testing shows spiruchostatin A to be a potent HDAC inhibitor. The synthetic route is suitable for the preparation of novel spiruchostatin and FK228 analogues.
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Published date: 2004
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Local EPrints ID: 465319
URI: http://eprints.soton.ac.uk/id/eprint/465319
PURE UUID: f3513652-1474-46d5-99c4-4175e9581f55
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Date deposited: 05 Jul 2022 00:37
Last modified: 16 Mar 2024 20:06
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Author:
Alexander Yurek-George
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