Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2)
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- 作者：Richard W. Heidebrecht Jr. ; Melissa Chenard ; Joshua Close ; William K. Dahlberg ; Judith Fleming ; Jonathan B. Grimm ; Julie E. Hamill ; Andreas Harsch ; Brian B. Haines ; Bethany Hughes ; Astrid M. Kral ; Ric
- 关键词：Pharmacokinetics ; Selective histone deacetylase inhibitor ; Zolinza ; Xenograft ; Phosphorus-containing therapeutic
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 April 2009
- 年：2009
- 卷：19
- 期：7
- 页码：2053-2058
- 全文大小：1334 K
文摘
We report the preparation and structure–activity relationships of phosphorus-containing histone deacetylase inhibitors. A strong trend between decreasing phosphorus functional group size and superior mouse pharmacokinetic properties was identified. In addition, optimized candidates showed tumor growth inhibition in xenograft studies.