发现新型 N-(2-嘧啶基氨基)苯甲酰胺衍生物作为有效的 Hedgehog 信号通路抑制剂。
The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors.
机构信息
Jiangsu Simcere Pharmaceutical Co. Ltd, Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, No. 699-18, Xuan Wu District, Nanjing 210042, PR China.
出版信息
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6777-83. doi: 10.1016/j.bmcl.2013.10.022. Epub 2013 Oct 17.
Hedgehog signaling pathway inhibitors are emerging as new therapeutic intervention against cancer. A novel series of N-(2-pyrimidinylamino) benzamide derivatives as hedgehog signaling pathway inhibitors were designed and synthesized. Most compounds presented significant inhibitory effect on hedgehog signaling pathway, among which 21 compounds exhibited more potent than vismodegib. Furthermore, compound 6a showed moderate pharmacokinetic properties in vivo, representing a promising lead compound for further exploration.
Hedgehog 信号通路抑制剂作为一种新的抗癌治疗方法正在兴起。设计并合成了一系列新型的 N-(2-嘧啶氨基)苯甲酰胺衍生物作为 Hedgehog 信号通路抑制剂。大多数化合物对 Hedgehog 信号通路表现出显著的抑制作用，其中 21 种化合物的抑制作用强于 vismodegib。此外，化合物 6a 在体内具有中等的药代动力学特性，代表了进一步探索的有前途的先导化合物。
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