Preparation of 6-substituted quinoxaline JSP-1 inhibitors by microwave accelerated nucleophilic substitution.
A small library of 6-aminoquinoxalines has been prepared by nucleophilic substitution of 6-fluoroquinoxaline with amines and nitrogen-containing heterocycles under computer-controlled microwave irradiation. Some compounds were found to be potent inhibitors of JNK Stimulatory Phosphatase-1 (JSP-1) in an in vitro biological assay.
Zhang
Li
L
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. zhangli@mail.shcnc.ac.cn
Qiu
Beiying
B
Li
Xin
X
Wang
Xin
X
Li
Jingya
J
Zhang
Yongliang
Y
Liu
Jian
J
Li
Jia
J
Shen
Jingkang
J
D000588:Amines / Q000737:chemistry; D054637:Dual-Specificity Phosphatases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000737:chemistry; D006801:Humans; D008872:Microwaves; D054639:Mitogen-Activated Protein Kinase Phosphatases / Q000037:antagonists & inhibitors*; D008956:Models, Chemical; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000588:Amines; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D011810:Quinoxalines; D054639:Mitogen-Activated Protein Kinase Phosphatases; C442824:DUSP22 protein, human; D054637:Dual-Specificity Phosphatases