Shiraishi T, Domoto T, Imai N, Shimada Y, Watanabe K
Biochem Biophys Res Commun. 1987 Aug 31;147(1):322-8. doi: 10.1016/s0006-291x(87)80124-9.
Several newly synthesized 4-hydroxycinnamamide derivatives such as 3-(3',5'-di-isopropyl-4'-hydroxybenzylidene)-2-oxindol (ST 280), 3-(3',5'-di-methylthiomethyl-4'-hydroxybenzylidene)-2-oxindole (ST 458), alpha-cyano-3-ethoxy-4-hydroxy-5-phenylthiomethylcinnamamide (ST 638) and 3-(3'-ethoxy-4'-hydroxy-5'-phenylthiomethylbenzylidene)-2-pyrol idinone (ST 642) were found to inhibit tyrosine-specific protein kinase activity of the epidermal growth factor (EGF) receptor with IC50 values of 0.44 microM, 0.44 microM, 0.37 microM and 0.85 microM, respectively. None of them showed inhibitory effect on the enzyme activities of serine- and/or threonine-specific protein kinases such as cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase C, casein kinase I and casein kinase II. In addition, none of them had effect on Na+/K+-ATPase or 5'-nucleotidase. The results suggest that the compound ST 280, ST 458, ST 638 and ST 642 are potent and specific inhibitors of tyrosine-specific protein kinase.
已发现几种新合成的4-羟基肉桂酰胺衍生物，如3-(3',5'-二异丙基-4'-羟基亚苄基)-2-氧代吲哚(ST 280)、3-(3',5'-二甲基硫代甲基-4'-羟基亚苄基)-2-氧代吲哚(ST 458)、α-氰基-3-乙氧基-4-羟基-5-苯基硫代甲基肉桂酰胺(ST 638)和3-(3'-乙氧基-4'-羟基-5'-苯基硫代甲基亚苄基)-2-吡咯烷酮(ST 642)，它们对表皮生长因子(EGF)受体的酪氨酸特异性蛋白激酶活性具有抑制作用，IC50值分别为0.44微摩尔/升、0.44微摩尔/升、0.37微摩尔/升和0.85微摩尔/升。它们均未对丝氨酸和/或苏氨酸特异性蛋白激酶如环磷酸腺苷依赖性蛋白激酶、Ca2+/磷脂依赖性蛋白激酶C、酪蛋白激酶I和酪蛋白激酶II的酶活性表现出抑制作用。此外，它们均对Na+/K+-ATP酶或5'-核苷酸酶无影响。结果表明，化合物ST 280、ST 458、ST 638和ST 642是酪氨酸特异性蛋白激酶的有效且特异性抑制剂。
