Journal
CANCER LETTERS
Volume 328, Issue 1, Pages 152-159Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.canlet.2012.08.020
Keywords
PI3K inhibitor; Anti-cancer drug; Apoptosis; Angiogenesis
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Funding
- National R&D Program for Cancer Control [1020250]
- Ministry of Health & Welfare, and National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2012-0002988, 2012-0003009, 2011-0016436, 2011-0020322]
- Inha University Grant
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We synthesized a novel imidazopyridine analogue, a PI3K alpha inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G(2)/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1 alpha and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro. Furthermore. HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Therefore, HS-173 is considered as a novel drug candidate to treat cancer patients. (C) 2012 Elsevier Ireland Ltd. All rights reserved.
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