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Pyrrole‐Based Hydroxamates and 2‐Aminoanilides: Histone Deacetylase Inhibition and Cellular Activities
Author(s) -
Valente Sergio,
Conte Mariarosaria,
Tardugno Maria,
Massa Silvio,
Nebbioso Angela,
Altucci Lucia,
Mai Antonello
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900082
Subject(s) - hdac1 , hdac4 , hdac6 , histone deacetylase , pyrrole , histone deacetylase 2 , recombinant dna , histone deacetylase 5 , hdac10 , chemistry , histone , hdac11 , biochemistry , cancer research , biology , gene , organic chemistry
Pyrrole‐based HDAC inhibitors : Pyrrolyl‐hydroxamates ( 3 a – g ) and 2‐aminoanilides ( 4 a – g ) derived from the class II‐selective histone deacetylase (HDAC) inhibitor MC1568 ( 1 ) were prepared and tested against human recombinant HDAC1, HDAC4, and HDAC6. Unlike compound 1 , most of the tested compounds inhibited both HDAC1 and HDAC6, and were less potent or completely inactive against HDAC4. Consistent with their high HDAC1/HDAC6 inhibition, compounds 3 a and 3 b induced>20 % cell death in U937 cells at 1 μ m.