2. Academic Validation
  3. Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor

Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor

  • Bioorg Med Chem. 2011 Jun 15;19(12):3702-8. doi: 10.1016/j.bmc.2010.12.024.
Daisuke Ogasawara 1,  Takayoshi Suzuki,  Koshiki Mino,  Rie Ueda,  Mohammed Naseer Ahmed Khan,  Takuya Matsubara,  Koichi Koseki,  Makoto Hasegawa,  Ryuzo Sasaki,  Hidehiko Nakagawa,  Tamio Mizukami,  Naoki Miyata
Affiliations

Affiliation

  • 1 Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Nagoya, Aichi 467-8603, Japan.
PMID: 21227703 DOI: 10.1016/j.bmc.2010.12.024
Abstract

Optically active (1S,2R)-NCL-1 and (1R,2S)-NCL-1 were synthesized and evaluated for their lysine-specific demethylase 1 inhibitory activity and cell growth inhibitory activity. In Enzyme assays, the (1S,2R)-isomer was approximately four times more potent than the (1R,2S)-isomer. In cell growth inhibition assays, the two isomers showed similar activity in HEK293 cells and SH-SY5Y cells, whereas the (1S,2R)-isomer showed approximately four times more potent activity than the (1R,2S)-isomer in HeLa cells.

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