Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2).

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Bioorganic & Medicinal Chemistry Letters. 2009 Apr 1;19(7):2053-8. doi: 10.1016/j.bmcl.2009.02.009

Heidebrecht RW, Chenard M, Close J, Dahlberg WK, Fleming J, Grimm JB, Hamill JE, Harsch A, Haines BB, Hughes B, Kral AM, Middleton RE, Mushti C, Ozerova N, Szewczak AA, Wang H, Wilson K, Witter DJ, Secrist JP, Miller TA

Note: Research in this publication was not performed at Janelia.

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Abstract

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.

PMID: 19268585 [PubMed - indexed for MEDLINE]

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Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2).

Note: Research in this publication was not performed at Janelia.

Abstract

PMID: 19268585 [PubMed - indexed for MEDLINE]

Janelia Authors