新型3H-咪唑并[4,5-b]吡啶衍生物作为选择性mTOR抑制剂的设计、合成及生物学评价
Design, synthesis and biological evaluation of novel 3H-imidazole [4,5-b] pyridine derivatives as selective mTOR inhibitors.
作者信息
Zhang Lingzhi, Bu Tantan, Bao Xiaobo, Liang Tingting, Ge Yiran, Xu Yungen, Zhu Qihua
机构信息
Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China.
Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 21009, China.
出版信息
Bioorg Med Chem Lett. 2017 Aug 1;27(15):3395-3398. doi: 10.1016/j.bmcl.2017.06.010. Epub 2017 Jun 3.
A series of 3H-imidazo [4,5-b] pyridines derivatives were designed and synthesized as selective mTOR inhibitors. The systematic optimization of the molecules resulted in the identification of two compounds 10d and 10n with nanomolar mTOR inhibitory activity and selectivity over PI3Kα. Besides, compounds 10d and 10n demonstrated attractive potency against human breast cancer cells (MCF-7) and human ovarian cancer cell (A2780).
设计并合成了一系列3H-咪唑并[4,5-b]吡啶衍生物作为选择性mTOR抑制剂。对这些分子进行系统优化后，鉴定出两种化合物10d和10n，它们具有纳摩尔级的mTOR抑制活性，且对PI3Kα具有选择性。此外，化合物10d和10n对人乳腺癌细胞（MCF-7）和人卵巢癌细胞（A2780）显示出有吸引力的活性。
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