Design, synthesis, enzyme inhibition, and tumor cell growth inhibition of 2-anilinobenzamide derivatives as SIRT1 inhibitors

Takayoshi Suzuki; Keiko Imai; Erika Imai; Shinsuke Iida; Ryuzo Ueda; Hiroki Tsumoto; Hidehiko Nakagawa; Naoki Miyata

doi:10.1016/j.bmc.2009.07.001

Design, synthesis, enzyme inhibition, and tumor cell growth inhibition of 2-anilinobenzamide derivatives as SIRT1 inhibitors

Bioorg Med Chem. 2009 Aug 15;17(16):5900-5. doi: 10.1016/j.bmc.2009.07.001. Epub 2009 Jul 7.

Authors

Takayoshi Suzuki¹, Keiko Imai, Erika Imai, Shinsuke Iida, Ryuzo Ueda, Hiroki Tsumoto, Hidehiko Nakagawa, Naoki Miyata

Affiliation

¹ Nagoya City University, Tanabe-dori, Mizuho-ku, Aichi, Japan. suzuki@phar.nagoya-cu.ac.jp

PMID: 19616958
DOI: 10.1016/j.bmc.2009.07.001

Abstract

A series of 2-anilinobenzamide derivatives were designed, synthesized and evaluated for their SIRT1-inhibitory activity. Among these, compounds 3 and 5 inhibited SIRT1 activity in enzyme assays and suppressed the growth of Daudi and HCT116 cells.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Benzamides / chemical synthesis*
Benzamides / chemistry*
Benzamides / pharmacology
Biphenyl Compounds / chemical synthesis*
Biphenyl Compounds / chemistry
Biphenyl Compounds / pharmacology
Cell Line, Tumor
Computer Simulation
Drug Design
Growth Inhibitors / chemical synthesis*
Growth Inhibitors / chemistry
Growth Inhibitors / pharmacology
HCT116 Cells
Humans
Protein Structure, Tertiary
Sirtuin 1
Sirtuins / antagonists & inhibitors*
Sirtuins / metabolism

Substances

2-(3-phenoxyphenylamino)benzamide
2-(biphenyl-3-ylamino)benzamide
Antineoplastic Agents
Benzamides
Biphenyl Compounds
Growth Inhibitors
benzamide
SIRT1 protein, human
Sirtuin 1
Sirtuins