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An expedient multi‐component synthesis of pyridinyl‐spirooxindoles and their effect on proliferation of lung cancer A549 cells
Author(s) -
Yan Liang,
Wu Xu,
Zhang Yizongheng,
Sankaran Mathan,
Xu Lei,
Ling Liefeng,
Wang Yi,
Jiang Yuxin,
Ma Jinzhu,
Kong Lingyu
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.4114
Subject(s) - chemistry , a549 cell , pi3k/akt/mtor pathway , protein kinase b , cell growth , phosphorylation , cell culture , in vitro , western blot , lung cancer , cancer research , microbiology and biotechnology , biochemistry , signal transduction , medicine , biology , gene , genetics
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 IC 50 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.