Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2

…, A Madriaga, H Abdelkarim, RB Van Breemen…

Index: Vaidya, Aditya Sudheer; Karumudi, Bhargava; Mendonca, Emma; Madriaga, Antonett; Abdelkarim, Hazem; Van Breemen, Richard B.; Petukhov, Pavel A. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5025 - 5030

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Citation Number: 12

Abstract

The design, modeling, synthesis, biological evaluation of a novel series of photoreactive benzamide probes for class I HDAC isoforms is reported. The probes are potent and selective for HDAC1 and 2 and are efficient in crosslinking to HDAC2 as demonstrated by photolabeling experiments. The probes exhibit a time-dependent inhibition of class I HDACs. The inhibitory activities of the probes were influenced by the positioning of the ...