Cushman M, Nagarathnam D, Geahlen R L
Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.
J Nat Prod. 1991 Sep-Oct;54(5):1345-52. doi: 10.1021/np50077a018.
An array of hydroxylated flavones and related compounds was synthesized and evaluated for inhibition of the in vitro protein-tyrosine kinase activity of p56lck, an enzyme that is thought to play a key role in mediating signal transduction from the CD4 receptor during lymphocyte activation. In general, the most active compounds had hydroxyl groups on both the A and C rings. At least two hydroxyl groups were required for good inhibitory activity, and the relative positions of these groups played an important role in determining potency. Compounds without hydroxyl groups were inactive as inhibitors.
合成了一系列羟基黄酮及相关化合物，并对其抑制p56lck体外蛋白酪氨酸激酶活性的能力进行了评估。p56lck是一种酶，被认为在淋巴细胞激活过程中介导CD4受体信号转导方面发挥关键作用。一般来说，活性最强的化合物在A环和C环上都有羟基。良好的抑制活性需要至少两个羟基，且这些羟基的相对位置在决定效力方面起着重要作用。没有羟基的化合物作为抑制剂没有活性。
