| Autor: |
H, Chen, G, Bashiardes, P, Mailliet, A, Commercon, F, Sounigo, J, Boiziau, F, Parker, B, Tocque, B P, Roques, C, Garbay |
| Rok vydání: |
1996 |
| Předmět: |
|
| Zdroj: |
Anti-cancer drug design. 11(1) |
| ISSN: |
0266-9536 |
| Popis: |
In order to obtain non-degradable and more potent protein-tyrosine kinase inhibitors, derived from the 5-(2,5-dihydroxybenzyl)-aminosalicylates already described, we have developed a new series of 5-(2,5-dihydroxybenzyl)phenylamines. The compounds, diversely substituted on the phenyl ring by alcohol, nitrile, ether, ketone, amide and thioamide groups, were tested for their ability to inhibit epidermal growth factor (EGF) receptor-associated tyrosine kinase activity in vitro. They inhibit the phosphorylation of the peptide substrate RR-Src by the EGF receptor purified from ER 22 cells, with IC50 values in the range 0.02-0.45 microns. Several of these compounds inhibit EGF-dependent DNA synthesis in ER 22 cells with IC50 values of around 1 micron and furthermore their inhibition has been found to be specific for various protein kinases. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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