Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 8, Pages 1122-1127Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00084
Keywords
HDAC6; isoform-selective; 2,4-imidazolinedione; antiproliferative; apoptosis
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Funding
- National Natural Science Foundation of China [81874288, 21672127]
- Key Research and Development Project of Shandong Province [2017CXGC1401]
- Fundamental Research Funds of Shandong University [2019GN045]
- Joint Research Funds for Shandong University and Karolinska Institute [SDU-KI-2019-06]
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Histone deacetylase 6 (HDAC6) has emerged as a promising drug target for various human diseases, including diverse neurodegenerative diseases and cancer. Herein, we reported a series of 2,4-imidazolinedione derivatives as novel HDAC6 isoform-selective inhibitors based on structure-based drug design. Most target compounds exhibit good profiles in a preliminary screening concerning HDAC6 inhibitory activities. Moreover, the most active compound 10c increases the acetylation level of alpha-tubulin with little effect on the acetylation of histone H3. Further biological evaluation suggested that potent compound 10c, which possesses good antiproliferative activity, could induce apoptosis in HL-60 cell by activating caspase 3.
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