Müller Christa E, Iqbal Jamshed, Baqi Younis, Zimmermann Herbert, Röllich Anita, Stephan Holger
Pharmaceutical Institute, Pharmaceutical Sciences Bonn (PSB), University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.
Bioorg Med Chem Lett. 2006 Dec 1;16(23):5943-7. doi: 10.1016/j.bmcl.2006.09.003. Epub 2006 Sep 25.
Polyoxotungstates were identified as potent inhibitors of NTPDases1, 2, and 3. The most potent compound was K(6)H(2)[TiW(11)CoO(40)], exhibiting K(i) values of 0.140 microM (NTPDase1), 0.910 microM (NTPDase2), and 0.563 microM (NTPDase3). One of the compounds, (NH(4))(18)[NaSb(9)W(21)O(86)], was selective for NTPDases2 and 3 versus NTPDase1. NTPDase inhibition might contribute to the described biological effects of polyoxometalates, including their anti-cancer activity.
多氧钨酸盐被鉴定为NTPDases1、2和3的有效抑制剂。最有效的化合物是K(6)H(2)[TiW(11)CoO(40)]，其对NTPDase1的抑制常数（Ki）值为0.140微摩尔，对NTPDase2为0.910微摩尔，对NTPDase3为0.563微摩尔。其中一种化合物(NH(4))(18)[NaSb(9)W(21)O(86)]对NTPDases2和3具有相对于NTPDase1的选择性。NTPDase抑制作用可能有助于多金属氧酸盐所描述的生物学效应，包括它们的抗癌活性。
