Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

Ubaldina Galli; Ornella Mesenzani; Camilla Coppo; Giovanni Sorba; Pier Luigi Canonico; Gian Cesare Tron; Armando A. Genazzani

doi:10.1016/j.ejmech.2012.07.001

Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

Ubaldina Galli
, Ornella Mesenzani
, Camilla Coppo
, Giovanni Sorba
, Pier Luigi Canonico
, Gian Cesare Tron
, Armando A. Genazzani

Department of Pharmaceutical Sciences

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

Abstract

As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.

Original language	English
Pages (from-to)	58-66
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	55
DOIs	https://doi.org/10.1016/j.ejmech.2012.07.001
Publication status	Published - Sept 2012

Keywords

Histone deacetylase
Isostere
N-Unsubstituted-1,2, 3-triazolyl pyridine
Rigid analogues
Sirtuins

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10.1016/j.ejmech.2012.07.001

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title = "Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2",

abstract = "As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.",

keywords = "Histone deacetylase, Isostere, N-Unsubstituted-1,2, 3-triazolyl pyridine, Rigid analogues, Sirtuins",

author = "Ubaldina Galli and Ornella Mesenzani and Camilla Coppo and Giovanni Sorba and Canonico, \{Pier Luigi\} and Tron, \{Gian Cesare\} and Genazzani, \{Armando A.\}",

note = "Funding Information: Financial support from Universit{\`a} del Piemonte Orientale and AIRC ( IG10509 )",

year = "2012",

month = sep,

doi = "10.1016/j.ejmech.2012.07.001",

language = "English",

volume = "55",

pages = "58--66",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

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T1 - Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

AU - Galli, Ubaldina

AU - Mesenzani, Ornella

AU - Coppo, Camilla

AU - Sorba, Giovanni

AU - Canonico, Pier Luigi

AU - Tron, Gian Cesare

AU - Genazzani, Armando A.

N1 - Funding Information: Financial support from Università del Piemonte Orientale and AIRC ( IG10509 )

PY - 2012/9

Y1 - 2012/9

N2 - As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.

AB - As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.

KW - Histone deacetylase

KW - Isostere

KW - N-Unsubstituted-1,2, 3-triazolyl pyridine

KW - Rigid analogues

KW - Sirtuins

UR - https://www.scopus.com/pages/publications/84865721413

U2 - 10.1016/j.ejmech.2012.07.001

DO - 10.1016/j.ejmech.2012.07.001

M3 - Article

SN - 0223-5234

VL - 55

SP - 58

EP - 66

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

Abstract

Keywords

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