Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.

Abstract:

:Two natural piperamides (piperlonguminine and refrofractamide A) and their derivatives were synthesized and evaluated for inhibitory activity against histone deacetylases, as well as the HCT-116 human colon cancer cell line. The preliminary structure activity relationship was discussed. Compounds featuring a hydroxamic acid moiety exhibited moderate HDAC activity and in vitro cytotoxicity.

journal_name

Bioorg Med Chem Lett

authors

Luo Y,Liu HM,Su MB,Sheng L,Zhou YB,Li J,Lu W

doi

10.1016/j.bmcl.2011.06.046

subject

Has Abstract

pub_date

2011-08-15 00:00:00

pages

4844-6

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00829-8

journal_volume

21

pub_type

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