TY - JOUR
T1 - Search for a novel SIRT1 activator
T2 - Structural modification of SRT1720 and biological evaluation
AU - Matsuya, Yuji
AU - Kobayashi, Yuta
AU - Uchida, Sayumi
AU - Itoh, Yukihiro
AU - Sawada, Hideyuki
AU - Suzuki, Takayoshi
AU - Miyata, Naoki
AU - Sugimoto, Kenji
AU - Toyooka, Naoki
PY - 2013/9/1
Y1 - 2013/9/1
N2 - Syntheses and biological evaluation of novel SRT1720 derivatives are described in search for new candidates of SIRT1 activator. Several parts of the SRT1720 structure, including piperazine moiety, quinoxaline ring on the amide group, and position of the amide function, were modified, and the assay results indicated that transfer of the ortho amide-substituent regarding to the imidazo[1,2-b]thiazole core onto the meta position resulted in improvement of SIRT1 activation ability. Modeling analyses of SRT1720 and the most potent derivative bound to model complex of SIRT1 with peptide substrate were also performed.
AB - Syntheses and biological evaluation of novel SRT1720 derivatives are described in search for new candidates of SIRT1 activator. Several parts of the SRT1720 structure, including piperazine moiety, quinoxaline ring on the amide group, and position of the amide function, were modified, and the assay results indicated that transfer of the ortho amide-substituent regarding to the imidazo[1,2-b]thiazole core onto the meta position resulted in improvement of SIRT1 activation ability. Modeling analyses of SRT1720 and the most potent derivative bound to model complex of SIRT1 with peptide substrate were also performed.
KW - Chemical synthesis
KW - Docking study
KW - Structural modification
UR - http://www.scopus.com/inward/record.url?scp=84881376738&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2013.06.070
DO - 10.1016/j.bmcl.2013.06.070
M3 - 学術論文
C2 - 23876989
AN - SCOPUS:84881376738
SN - 0960-894X
VL - 23
SP - 4907
EP - 4910
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 17
ER -