Department of Molecular Medicine, Beckman Research Institute at City of Hope, Duarte, CA 91010, United States.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):83-6. doi: 10.1016/j.bmcl.2009.11.036. Epub 2009 Nov 14.
A series of ageladine A analogs that include 2-aminoimidazo[4,5-c]azepines (seven-membered rings) and 2-amino-3H-imidazo[4,5-c]pyridine (six-membered rings) derivatives were synthesized and evaluated for their anticancer effects against several human cancer cell lines and MMP-2 inhibition in vitro. Only compounds possessing the aromatic azepine (seven-membered ring) core showed anticancer activity with IC(50) values in the low micromolar range.
一系列包含 2-氨基咪唑并[4,5-c]氮杂环庚烷(七元环)和 2-氨基-3H-咪唑并[4,5-c]吡啶(六元环)衍生物的阿格拉定 A 类似物被合成,并评估了它们对几种人癌细胞系的抗癌作用和 MMP-2 的体外抑制作用。只有具有芳香氮杂环庚烷(七元环)核心的化合物表现出抗癌活性,IC50 值在低微摩尔范围内。