Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

Yu Luo; Hao Min Liu; Ming Bo Su; Li Sheng; Yu Bo Zhou; Jia Li; Wei Lu

doi:10.1016/j.bmcl.2011.06.046

Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

Yu Luo
, Hao Min Liu
, Ming Bo Su
, Li Sheng
, Yu Bo Zhou
, Jia Li^*
, Wei Lu

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

East China Normal University
CAS - Shanghai Institute of Materia Medica

Research output: Contribution to journal › Article › peer-review

13 Scopus citations

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.

Original language	English
Pages (from-to)	4844-4846
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	16
DOIs	https://doi.org/10.1016/j.bmcl.2011.06.046
State	Published - 15 Aug 2011

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

HDAC
Piperlonguminine
Refrofractamide A

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10.1016/j.bmcl.2011.06.046

Cite this

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title = "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.",

keywords = "HDAC, Piperlonguminine, Refrofractamide A",

author = "Yu Luo and Liu, \{Hao Min\} and Su, \{Ming Bo\} and Li Sheng and Zhou, \{Yu Bo\} and Jia Li and Wei Lu",

year = "2011",

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pages = "4844--4846",

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T1 - Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

AU - Luo, Yu

AU - Liu, Hao Min

AU - Su, Ming Bo

AU - Sheng, Li

AU - Zhou, Yu Bo

AU - Li, Jia

AU - Lu, Wei

PY - 2011/8/15

Y1 - 2011/8/15

N2 - 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.

AB - 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.

KW - HDAC

KW - Piperlonguminine

KW - Refrofractamide A

UR - https://www.scopus.com/pages/publications/79960896421

U2 - 10.1016/j.bmcl.2011.06.046

DO - 10.1016/j.bmcl.2011.06.046

M3 - 文章

C2 - 21745740

AN - SCOPUS:79960896421

SN - 0960-894X

VL - 21

SP - 4844

EP - 4846

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

Abstract

UN SDGs

Keywords

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