| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379370 | Bioorganic & Medicinal Chemistry Letters | 2005 | 6 Pages |
Abstract
Starting from the pharmacophore model for HDAC inhibitor design, a novel series of hydroxamates bearing a uracil moiety as connecting unit (CU) has been prepared and tested. Almost all compounds exhibited HDAC inhibiting activity at low nanomolar concentrations, the N-hydroxy-6-(3,4-dihydro-4-oxo-6-benzyl- and -6-phenyl-2-pyrimidinylthio)hexanamides 1d and 1l being more potent than SAHA in enzymatic assays. Such compounds also caused hyperacetylation in NIH3T3 cell core histones and were endowed with interesting antiproliferative and cytodifferentiating effects in human leukemia (HL-60) cells.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Antonello Mai, Silvio Massa, Dante Rotili, Riccardo Pezzi, Patrizia Bottoni, Roberto Scatena, Joachim Meraner, Gerald Brosch,