发现并研究 4-(2-芳基吡啶并[3',2':3,4]吡咯并[1,2-f][1,2,4]三嗪-4-基)吗啉衍生物作为新型 PI3K 抑制剂的生物活性。
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China.
出版信息
Bioorg Med Chem Lett. 2012 Jan 1;22(1):339-42. doi: 10.1016/j.bmcl.2011.11.003. Epub 2011 Nov 9.
PI3K is a promising therapeutic target for cancer. With PI-103 as the lead compound, we designed and synthesized 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl)morpholine derivatives. 9, 10a, 10d, 10e had the IC(50) against PI3Kα comparable with PI-103. All of the compounds showed selectivity over 15 tested protein kinases and anti-proliferative activity at micromolar concentration against several cancer cell lines.
PI3K 是癌症治疗的一个有前景的靶点。以 PI-103 为先导化合物，我们设计并合成了 4-(2-芳基吡啶并[3',2':3,4]吡咯并[1,2-f][1,2,4]三嗪-4-基)吗啉衍生物。9、10a、10d、10e 对 PI3Kα 的抑制活性与 PI-103 相当。所有化合物对 15 种测试蛋白激酶表现出选择性，并且在微摩尔浓度下对几种癌细胞系具有抗增殖活性。
Zotero 插件