Department of Biomedical Sciences, College of Medicine, Inha University, 3-ga, Sinheung-dong, Jung-gu, Incheon 400-712, Republic of Korea.
Cancer Lett. 2013 Jan 1;328(1):152-9. doi: 10.1016/j.canlet.2012.08.020. Epub 2012 Aug 26.
We synthesized a novel imidazopyridine analogue, a PI3Kα 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-1α 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.
我们合成了一种新型的咪唑并吡啶类似物，PI3Kα 抑制剂 HS-173，并研究了其在人类癌细胞中的抗癌能力。HS-173 抑制了 PI3K 信号通路，并对癌细胞表现出抗增殖作用。此外，HS-173 诱导细胞周期停滞在 G2/M 期并诱导细胞凋亡。此外，HS-173 降低了在血管生成中起重要作用的 HIF-1α 和 VEGF 的表达。这一作用通过体外管形成和迁移试验得到证实。此外，HS-173 减少了小鼠 Matrigel plugs 实验中的血管形成。因此，HS-173 被认为是一种治疗癌症患者的新型候选药物。
