A novel imidazopyridine PI3K inhibitor with anticancer activity in non-small cell lung cancer cells

Lee,Hyunseung; Kim,Soo  Jung; Jung,Kyung  Hee; Son,Mi  Kwon; Yan,Hong  Hua; Hong,Sungwoo; Hong,Soon-Sun

doi:10.3892/or.2013.2499

A novel imidazopyridine PI3K inhibitor with anticancer activity in non-small cell lung cancer cells

Authors:
- Hyunseung Lee
- Soo Jung Kim
- Kyung Hee Jung
- Mi Kwon Son
- Hong Hua Yan
- Sungwoo Hong
- Soon-Sun Hong
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Affiliations: Department of Drug Development, College of Medicine, Inha University, Sinheung‑dong, Jung‑gu, Incheon 400-712, Republic of Korea, Department of Chemistry, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 305-701, Republic of Korea
Published online on: May 27, 2013 https://doi.org/10.3892/or.2013.2499
Pages: 863-869

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Abstract

Lung cancer is the leading cause of cancer-related mortality in the world, and non-small cell lung cancer (NSCLC) accounts for approximately 85% of all cases. Since more than 60% of NSCLC cases express the epidermal growth factor receptor (EGFR), EGFR tyrosine kinase inhibitors are used to treat NSCLC. However, due to the acquired resistance associated with EGFR-targeted therapy, other strategies for the treatment of NSCLC are urgently needed. Therefore, we investigated the anticancer effects of a novel phosphatidylinositol 3-kinase α (PI3Kα) inhibitor, HS-173, in human NSCLC cell lines. HS-173 demonstrated anti-proliferative effects in NSCLC cells and effectively inhibited the PI3K signaling pathway in a dose‑dependent manner. In addition, it induced cell cycle arrest at G2/M phase as well as apoptosis. Taken together, our results demonstrate that HS-173 exhibits anticancer activities, including the induction of apoptosis, by blocking the PI3K/Akt/mTOR pathway in human NSCLC cell lines. We, therefore, suggest that this novel drug could potentially be used for targeted NSCLC therapy.

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