期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 15, 页码 5532-5539出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200577a
关键词
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资金
- National Nature Science Foundation of China [30772654, 36072541]
- National High Technology Research and Development Program of China (863 project) [2007AA02Z314]
- National Science and Technology Major Project [2009ZX09103-118]
- Ministry of Education of China
Histone deacetylase (HDAC) has emerged as an attractive target for the development of antitumor agents during the past decade. Previously tetrahydroisoquinoline-bearing hydroxamic acid analogue, ZYJ-25e (1), was identified and validated as a potent histone deacetylase inhibitor (HDACi) with marked in vitro and in vivo antitumor potency. In the present study, further modification of 1 led to another more potent, orally active HDACi, ZYJ-34c (4). Compared to FDA-approved drug suberoylanilide hydroxamic acid (SAHA), compound 4 exhibited higher in vivo antitumor potency in a human breast carcinoma (MDA-MB-231) xenograft model and in a mouse hepatoma-22 (H22) pulmonary metastasis model and similar in vivo antitumor potency in a human colon tumor (HCT116) xenograft model.
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