Phosphorus-based SAHA analogues as histone deacetylase inhibitors.

Journal Article (Journal Article)

[structure: see text] Three analogues of suberoyl anilide hydroxamic acid (SAHA) with phosphorus metal-chelating functionalities were synthesized as inhibitors of histone deacetylases (HDACs). The compounds showed weak activity for HeLa nuclear extracts (IC(50) = 0.57-6.1 mM), HDAC8 (IC(50) = 0.28-0.41 mM), and histone-deacetylase-like protein (HDLP, IC(50) = 0.33-1.9 mM), suggesting that the transition state of HDAC is not analogous to zinc proteases. Antiproliferative activity against A2780 cancer cells (IC(50) = 0.11-0.12 mM), comparable to SAHA (0.15 mM), was observed.

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Duke Authors

McCafferty, Dewey G.

Cited Authors

Kapustin, GV; Fejér, G; Gronlund, JL; McCafferty, DG; Seto, E; Etzkorn, FA

Published Date

August 2003

Published In

Organic Letters

Volume / Issue

5 / 17

Start / End Page

3053 - 3056

PubMed ID

12916979

Electronic International Standard Serial Number (EISSN)

1523-7052

International Standard Serial Number (ISSN)

1523-7060

Digital Object Identifier (DOI)

10.1021/ol035056n

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