170455-85-3Relevant academic research and scientific papers
Hydroxamic acid derivative and JHDM inhibitor
-
, (2016/10/09)
PROBLEM TO BE SOLVED: To provide a compound capable of selectively inhibiting the function of JHDM, and a JHDM inhibitor. SOLUTION: This hydroxamic acid derivative expressed by formula (1a) [wherein, R1and R2are each independently alkyl which may have a branch; and (n) is an integer of ≥1] or general formula (1b) [wherein, ring X is a 3 to 8-membered saturated carbon ring; and (n) is an integer of ≥1], its pharmaceutically acceptable salt, hydrate, solvate or prodrug is provided. COPYRIGHT: (C)2011,JPOandINPIT
Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors
Hamada, Shohei,Suzuki, Takayoshi,Mino, Koshiki,Koseki, Koichi,Oehme, Felix,Flamme, Ingo,Ozasa, Hiroki,Itoh, Yukihiro,Ogasawara, Daisuke,Komaarashi, Haruka,Kato, Aiko,Tsumoto, Hiroki,Nakagawa, Hidehiko,Hasegawa, Makoto,Sasaki, Ryuzo,Mizukami, Tamio,Miyata, Naoki
experimental part, p. 5629 - 5638 (2010/10/03)
Selective inhibitors of Jumonji domain-containing protein (JMJD) histone demethylases are candidate anticancer agents as well as potential tools for elucidating the biological functions of JMJDs. On the basis of the crystal structure of JMJD2A and a homology model of JMJD2C, we designed and prepared a series of hydroxamate analogues bearing a tertiary amine. Enzyme assays using JMJD2C, JMJD2A, and prolyl hydroxylases revealed that hydroxamate analogue 8 is a potent and selective JMJD2 inhibitor, showing 500-fold greater JMJD2C-inhibitory activity and more than 9100-fold greater JMJD2C-selectivity compared with the lead compound N-oxalylglycine 2. Compounds 17 and 18, prodrugs of compound 8, each showed synergistic growth inhibition of cancer cells in combination with an inhibitor of lysine-specific demethylase 1 (LSD1). These findings suggest that combination treatment with JMJD2 inhibitors and LSD1 inhibitors may represent a novel strategy for anticancer chemotherapy.
Easy synthesis of unnatural siderophores
Zhu,Robin,Goasdoue,Goasdoue,Loupy,Galons
, p. 2515 - 2519 (2007/10/02)
N-Acetyl-N-benzyloxy-β-alanine was obtained by Michael addition of N-acetyl-N-benzyloxyamine on terbutylacrylate under solvent-free PTC conditions followed by elimination of the terbutyl group. Polyamines were acylated with N-acetyl-N-benzyloxy-β-alanine.
