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Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.

Abstract：

:Nonpeptidic chiral macrocycles were designed on the basis of an analogue of suberoylanilide hydroxamic acid (2) (SAHA, vorinostat) and evaluated against 11 histone deacetylase (HDAC) isoforms. The identification of critical amino acid residues highly conserved in the cap region of HDACs guided the design of the suberoyl-based macrocycles, which were expected to bear a maximum common substructure required to target the whole HDAC panel. A nanomolar HDAC inhibitory profile was observed for several compounds, which was comparable, if not superior, to that of 2. A promising cytotoxic activity was found for selected macrocycles against lung and colon cancer cell lines. Further elaboration of selected candidates led to compounds with an improved selectivity against HDAC6 over the other isozymes. Pair-fitting analysis was used to compare one of the best candidates with the natural tetrapeptide apicidin, in an effort to define a general pharmacophore that might be useful in the design of surrogates of peptidic macrocycles as potent and isoform-selective inhibitors.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Auzzas L,Larsson A,Matera R,Baraldi A,Deschênes-Simard B,Giannini G,Cabri W,Battistuzzi G,Gallo G,Ciacci A,Vesci L,Pisano C,Hanessian S

doi

10.1021/jm101092u

subject

Has Abstract

pub_date

2010-12-09 00:00:00

pages

8387-99

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

53

pub_type

杂志文章

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