title: 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.
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Chen
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Chai
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Ming-Bo
authors.initials: MB
authors.lastname: Su
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Yang-Ming
authors.initials: YM
authors.lastname: Zhang
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Xie
authors.affiliation: Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
authors.forename: Fa-Jun
authors.initials: FJ
authors.lastname: Nan
keywords: Histone deacetylase inhibitors; bisthiazole; largazole