6,7-二芳基-2,3,8,8a-四氢中氮茚-5(1H)-酮的合成、体外和体内细胞毒性
Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones.
作者信息
Kimball F Scott, Tunoori Ashok Rao, Victory Samuel F, Dutta Dinah, White Jonathan M, Himes Richard H, Georg Gunda I
机构信息
Department of Medicinal Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA.
出版信息
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4703-7. doi: 10.1016/j.bmcl.2007.05.103. Epub 2007 Jun 13.
Abstract
A 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one library was constructed and tested against the colon cancer cell line HCT-116 as an initial screen for cytotoxic properties. Of this library, the parent compound, in which the southern aromatic ring remains unsubstituted, and the northern aromatic ring carries a 4-methoxy group, exhibited the most potent cytotoxicity with an IC50 value of 0.39 microM and displayed promising activity in vivo in the NCI's mouse hollow fiber assay.
摘要
构建了一个6,7-二芳基-2,3,8,8a-四氢中氮茚-5(1H)-酮文库，并针对结肠癌细胞系HCT-116进行测试，作为细胞毒性特性的初步筛选。在该文库中，母体化合物（其中南部芳环未被取代，北部芳环带有一个4-甲氧基）表现出最强的细胞毒性，IC50值为0.39微摩尔，并且在美国国立癌症研究所的小鼠中空纤维试验中在体内显示出有前景的活性。
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