879216-06-5Relevant academic research and scientific papers
Design, synthesis, modeling, biological evaluation and photoaffinity labeling studies of novel series of photoreactive benzamide probes for histone deacetylase 2
Vaidya, Aditya Sudheer,Karumudi, Bhargava,Mendonca, Emma,Madriaga, Antonett,Abdelkarim, Hazem,Van Breemen, Richard B.,Petukhov, Pavel A.
scheme or table, p. 5025 - 5030 (2012/08/28)
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 aryl and alkyl azido groups necessary for photocrosslinking and attachment of the biotin tag. The probes inhibited the deacetylation of H4 in MDA-MB-231 cell line, indicating that they are cell permeable and target the nuclear HDACs.
Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases
Srinivasan, Rajavel,Uttamchandani, Mahesh,Yao, Shao Q.
, p. 713 - 716 (2007/10/03)
We have successfully designed and synthesized a small library of protein tyrosine phosphatase (PTP) inhibitors, in which the so-called "click chemistry" or Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction was carried out for rapid assembly of 66 different bidentate compounds. Subsequent in situ enzymatic screening revealed a potential PTP1B inhibitor (IC50 = 4.7 μM) which is 10-100 fold more potent than other PTPs.
