| Institution: | 1. Provincial Key Laboratory of Biological Macro-molecules Research, Wannan Medical College, Wuhu, Anhui, China;2. Provincial Key Laboratory of Biological Macro-molecules Research, Wannan Medical College, Wuhu, Anhui, China
Liang Yan and Xu Wu are contributed equally to this work.;3. First Clinical College, Southern Medical University, Guangzhou, Guangdong, China;4. Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry & Chemical Engineering, Nanjing University, Nanjing, China;5. Department of Pathogen Biology and Immunology, Jiaxing University College of Medicine, Jiaxing, Zhejiang, China |
| Abstract: | A series of new functionalized pyridinyl-spirooxindoles have been synthesized through three-component cyclization reactions. The selected compounds were screened for their in vitro antiproliferative activity against human lung cancer cell line A549. Among the candidate structures, compound 1o demonstrated maximum inhibitory activity against A549 cells with IC50 values of 28.38 μM. EdU (5-Ethynyl-2′- deoxyuridine, EdU) assay and cell colony formation test showed that cell proliferation of A549 cells was inhibited. In addition, Western blot analysis revealed that the phosphorylation levels of Akt, mTOR, 70S6, and S6 were down-regulated. Thus, these results indicated that 1o may inhibit the proliferation of A549 cells through inhibiting the phosphorylation levels of Akt, mTOR, 70S6, and S6. 1o may be developed as a potential antitumor agent for lung cancer treatment. |
