[Synthesis and biological activity of tyrosine protein kinase inhibitors].
Four classes of 25 tyrosine protein kinase (TPK) inhibitors were designed and synthesized. Compounds 1-10 were tested to inhibit TPK of HL-60 leukemia cell using 32P-ATP method, and some of them exhibit evident inhibitory activities. Their structure-activity relationship is similar to that of TPK inhibitors reported in literatures. Compounds 11-25 were tested to inhibit TPK of normal rat spleen cell using ELISA method and their SAR is different from that using 32P-ATP method.
Pang
S H
SH
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking, Union Medical College, Beijing 100050.
Guo
Z R
ZR
Liang
X T
XT
D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D013154:Spleen / Q000166:cytology / Q000378:metabolism; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D011505:Protein-Tyrosine Kinases