Biological Evaluation of New Largazole Analogues: Alteration of Macrocyclic Scaffold with Click Chemistry
Year: 2012
Type: article
Abstract: We report the design, synthesis, and biological evaluation of a new series of largazole analogues in which a 4-methylthiazoline moiety was replaced with a triazole and tetrazole ring, respectively. Compound 7 bearing a tetrazole ring was identified to show much better selectivity for HDAC1 over HDAC9 than largazole (10-fold). This work could serve as a foundation for further exploration of selective HDAC inhibitors using a largazole molecular scaffold.
Source: ACS Medicinal Chemistry Letters
DOI: 10.1021/ml300371t
Authors: Xianlin Li, Zhenchao Tu, Hua Li, Chunping Liu, Zheng Li, Qiao Sun, Yiwu Yao, Jinsong Liu, Sheng Jiang
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
Award: G2922681079
OpenAlex ID: W1979932558