Metachromins L-Q 及其相关类似物对受体酪氨酸激酶 EGFR 和 HER2 的抑制作用。
Inhibitory effects of metachromins L-Q and its related analogs against receptor tyrosine kinases EGFR and HER2.
机构信息
Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo 060-0812, Japan.
出版信息
Bioorg Med Chem Lett. 2013 Jan 1;23(1):117-8. doi: 10.1016/j.bmcl.2012.11.001. Epub 2012 Nov 10.
Metachromins are a series of sesquiterpenoid quinones isolated from Okinawan marine sponges. Inhibitory effects of metachromins L-Q (1-6), sesquiterpenoid quinones with an amino acid residue, and their related analogs (7-18) prepared from metachromins A (19) and C (20) against receptor tyrosine kinases EGFR and HER2 were investigated. Two analogs 11 and 12 showed relatively stronger inhibitory activity against EGFR, while metachromins L-Q (1-6) and seven analogs (8, 10, 11, and 15-18) showed inhibitory activities against HER2.
美拉托宁是从冲绳海洋海绵中分离得到的一系列倍半萜醌类化合物。对来源于美拉托宁 A（19）和 C（20）的美拉托宁 L-Q（1-6）、具有氨基酸残基的倍半萜醌类化合物及其相关类似物（7-18）对受体酪氨酸激酶 EGFR 和 HER2 的抑制作用进行了研究。两个类似物 11 和 12 对 EGFR 表现出相对较强的抑制活性，而美拉托宁 L-Q（1-6）和 7 个类似物（8、10、11 和 15-18）对 HER2 表现出抑制活性。
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