PTP-1B inhibitors: cyclopenta[d][1,2]-oxazine derivatives.
A series of novel cyclopenta[d][1,2]-oxazine derivatives was prepared and evaluated for their inhibitory activity toward protein tyrosine phosphatase 1B (PTP-1B). Compound 6s was found to be an inhibitor of PTP-1B with nanomolar IC(50) value and high level of selectivity over other recombinant phosphatases.
Cho
Sung Yun
SY
Bio-Organic Science Division, Korea Research Institute of Chemical Technology, 100 Jang-dong, Yuseong-gu, Daejeon 305-600, Republic of Korea.
Baek
Ji Yoen
JY
Han
Sang Sub
SS
Kang
Seung Kyu
SK
Ha
Jae Du
JD
Ahn
Jin Hee
JH
Lee
Jae Don
JD
Kim
Kwang Rok
KR
Cheon
Hyae Gyeong
HG
Rhee
Sang Dal
SD
Yang
Sung Don
SD
Yon
Gyu Hwan
GH
Pak
Chwang Siek
CS
Choi
Joong-Kwon
JK
D003517:Cyclopentanes / Q000138:chemical synthesis*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D010078:Oxazines / Q000138:chemical synthesis*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D003517:Cyclopentanes; D004791:Enzyme Inhibitors; D010078:Oxazines; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases