嘧啶并[5,4-e][1,2,4]三嗪-5,7(1H,6H)-二酮衍生物：它们对鱼藤酮毒性的细胞保护作用及其初步的 DMPK 性质。
Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: their cytoprotection effect from rotenone toxicity and preliminary DMPK properties.
机构信息
CytRx Corporation, 3030 Bunker Hill Street, Suite 101, San Diego, CA 92109, USA.
出版信息
Bioorg Med Chem Lett. 2009 Nov 1;19(21):6114-8. doi: 10.1016/j.bmcl.2009.09.021. Epub 2009 Sep 10.
PMID:19786349
Abstract
Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives exhibited potent cytoprotective effect from rotenone toxicity. Lead optimization focused on the CC50/EC50 ratio and DMPK properties led to the overall improvement of the compound profile of this series with high CC50/EC50 ratio (92 for 1f), good metabolic stability in rat microsomes and medium to high aqueous solubility.
摘要
嘧啶并[5,4-e][1,2,4]三嗪-5,7(1H,6H)-二酮衍生物表现出对鱼藤酮毒性的强大细胞保护作用。先导化合物优化的重点是 CC50/EC50 比值和 DMPK 性质，这导致该系列化合物的整体特性得到改善，具有高 CC50/EC50 比值（1f 为 92）、在大鼠微粒体中良好的代谢稳定性和中等至高的水溶解度。
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