(Chemical Equation Presented) 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 1m. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
Pyrrole-Based Hydroxamates and 2-Aminoanilides: Histone Deacetylase Inhibition and Cellular Activities / Mariarosaria, Conte; Maria, Tardugno; Silvio, Massa; Angela, Nebbioso; Lucia, Altucci; Mai, Antonello; Valente, Sergio. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 4:9(2009), pp. 1411-1415. [10.1002/cmdc.200900082]
Pyrrole-Based Hydroxamates and 2-Aminoanilides: Histone Deacetylase Inhibition and Cellular Activities
MAI, Antonello;VALENTE, Sergio
2009
Abstract
(Chemical Equation Presented) 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 1m. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
