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Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.

ABSTRACT: Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.

SUBMITTER: Chen F 

PROVIDER: S-EPMC4060935 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature

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Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.

Chen Fei F   Chai Hui H   Su Ming-Bo MB   Zhang Yang-Ming YM   Li Jia J   Xie Xin X   Nan Fa-Jun FJ  

ACS medicinal chemistry letters 20140404 6

Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice. ...[more]

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