期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 82, 期 2, 页码 125-130出版社
WILEY-BLACKWELL
DOI: 10.1111/cbdd.12144
关键词
antitumor; histone deacetylases; inhibitor; oral active; tetrahydroisoquinoline; valproic acid
资金
- National Scientific and Technological Major Project of Ministry of Science and Technology of China [2011ZX09401-015]
- National Natural Science Foundation of China [21172134]
- Doctoral Foundation of Ministry of Education of China [20110131110037]
- Independent Innovation Foundation of Shandong University, IIFSDU [2013GN013]
- National Cancer Institute of the National Institute of Health [R01CA163452]
In our previous study, we developed a novel series of tetrahydroisoquinoline-based hydroxamic acid derivatives as histone deacetylase inhibitors (Bioorg Med Chem, 2010, 18, 1761-1772; J Med Chem, 2011, 54, 2823-2838), among which, compound ZYJ-34c (1) was identified and validated as the most potent one with marked in vitro and in vivo antitumor potency (J Med Chem, 2011, 54, 5532-5539.). Herein, further modification in 1 afforded another oral active analog ZYJ-34v (2) with simplified structure and lower molecular weight. Biological evaluation of compound 2 showed efficacious inhibition against histone deacetylase 1, 2, 3, and 6, which was confirmed by Western blot analysis results. Most importantly, compound 2 exhibited similar even more potent in vitro and in vivo antitumor activities relative to the approved histone deacetylase inhibitor SAHA.
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