Abstract:
:Inhibitors of histone deacetylases (HDACs) are a promising class of anticancer agents that have an effect on gene regulation. The naturally occurring cyclic depsipeptide FK228 containing disulfide and Largazole possessing thioester functionalities act as pro-drugs and share the same HDAC inhibition mechanism in cell. Inspired from these facts, we have reported bicyclic tetrapeptide disulfide HDAC inhibitors resembling FK228 with potent activity and enhanced selectivity. In the present study, we report the design and synthesis of several mono and bicyclic tetrapeptide thioester HDAC inhibitors that share the inhibition mechanism similar to Largazole. Most of the compounds showed HDAC1 and HDAC4 inhibition and p21 promoting activity in nanomolar ranges. Among these the monocyclic peptides 1, 2 and bicyclic peptide, 4 are notable demanding more advanced research to be promising anticancer drug candidates.
journal_name
Amino Acidsjournal_title
Amino acidsauthors
Hoque MA,Islam MS,Islam MN,Kato T,Nishino N,Ito A,Yoshida Mdoi
10.1007/s00726-014-1800-5subject
Has Abstractpub_date
2014-10-01 00:00:00pages
2435-44issue
10eissn
0939-4451issn
1438-2199journal_volume
46pub_type
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