Synthesis and Evaluation of Aliphatic-chain Hydroxamates Capped with Osthole Derivatives as Histone Deacetylase Inhibitors

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標題:	Synthesis and Evaluation of Aliphatic-chain Hydroxamates Capped with Osthole Derivatives as Histone Deacetylase Inhibitors
作者:	Shih-Wei Chao (趙世偉) Ching-Chow Chen Chen-Yui Yang Yun-Chieh Lin Chia-Chun Yu Jih-Hwa Guh Chiao-I Kuo Ping Yang Chung-I Chang Wei-Jan Huang
日期:	2011
上傳時間:	2011-06-23 14:57:21 (UTC+8)
摘要:	Our previous studies have demonstrated that osthole, a Chinese herbal compound, could be incorporated into the hydroxycinnamide scaffold of LBH-589, a potent HDAC inhibitor, as an effective hydrophobic cap; the resulting compounds showed gnificant potency against several HDAC isoforms. Here, we presented a series of osthole derivatives fused with the aliphatic-hydroxamate core of suberoylanilide hydroxamic acid (SAHA), a clinically-approved HDAC inhibitor. Several compounds showed potent activity against nuclear HDACs comparable. Further assays against individual HDAC isoforms revealed that some compounds showed not only SAHA-like activity towards HDAC1, -4 and -6, they inhibited HDAC8 by log difference than SAHA and thus exhibited a broader HDAC inhibition spectrum. Among them, compound 6g showed multiple significant cellular effects towards human prostate cancer cells.
關聯:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
显示于类别:	[藥理學院] 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會

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