通过“点击化学”设计并合成一种新型的、构象受限的STAT3大环小分子抑制剂。
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.
作者信息
Chen Jianyong, Nikolovska-Coleska Zaneta, Yang Chao-Yie, Gomez Cindy, Gao Wei, Krajewski Krzysztof, Jiang Sheng, Roller Peter, Wang Shaomeng
机构信息
University of Michigan Comprehensive Cancer Center, Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48109, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3939-42. doi: 10.1016/j.bmcl.2007.04.096. Epub 2007 May 3.
STAT3 is a promising molecular target for the design of new anticancer drugs. In this paper, we report the design and synthesis of a conformationally constrained macrocyclic peptidomimetic 2 via click chemistry. Compound 2 was determined to bind to STAT3 with a K(i) value of 7.3 microM in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization.
信号转导和转录激活因子3（STAT3）是新型抗癌药物设计中一个很有前景的分子靶点。在本文中，我们报道了通过点击化学设计并合成构象受限的大环肽模拟物2。在基于竞争性荧光偏振的结合试验中，化合物2与STAT3结合的抑制常数（K(i)）值为7.3微摩尔，这表明它是一个有前景的初始先导化合物，可用于进一步优化。
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