新型7-氨基-5-甲基-1,6-萘啶-2(1H)-酮衍生物作为强效PI3K/mTOR双重抑制剂的鉴定
Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.
作者信息
Lin Songwen, Han Fangbin, Liu Peng, Tao Jing, Zhong Xuechao, Liu Xiujie, Yi Chongqin, Xu Heng
机构信息
PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No. 29 Life Science Park Road, Changping District, Beijing 102206, PR China.
PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No. 29 Life Science Park Road, Changping District, Beijing 102206, PR China.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):790-3. doi: 10.1016/j.bmcl.2013.12.112. Epub 2014 Jan 3.
Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors. Design, synthesis and structure activity relationship are reported.
抑制磷酸肌醇3-激酶（PI3K）/蛋白激酶B（AKT）/雷帕霉素哺乳动物靶点（mTOR）信号通路是癌症治疗中研究最为深入的方法之一。通过合理设计，确定了新型7-氨基-5-甲基-1,6-萘啶-2（1H）-酮衍生物作为有效的PI3K/mTOR双重抑制剂。本文报道了其设计、合成及构效关系。
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