Glioblastoma (GBM) are life-threatening tumors with a poor prognosis and low cure rates. GBMs are malignant brain tumors that develop from astrocytes. Most GBMs are not inherited and occur sporadically. GBM recurrence after standard treatment has led to the assessment of agents targeting the CXCR4 chemokine receptor as alternative drug target for much needed GBM therapeutics. In present study, a novel CXCR4 inhibitor modified with a picolinamide scaffold (CPZ1344) was designed and synthesized. Its anti-GBM function was then evaluated. Our results showed that CPZ1344 reduced the growth of GBM cells in a concentration dependent manner. The anti-GBM activity of CPZ1344 was due to alteration in GBM-cell morphology and apoptotic induction in GBM cells. CPZ1344 inhibited the migration and angiogenesis of U87 cells, led to cell cycle arrest in the G1 phase and inhibited CXCR4 signaling. These findings demonstrate the anticancer effects of CPZ1344 and its potential as a novel anti-GBM therapeutic.

胶质母细胞瘤（GBM）是一种危及生命的肿瘤，预后不良，治愈率低。 GBM 是由星形胶质细胞发展而来的恶性脑肿瘤。大多数 GBM 不是遗传性的，而是偶发性的。标准治疗后 GBM 复发导致人们对靶向 CXCR4 趋化因子受体的药物进行评估，作为急需的 GBM 治疗的替代药物靶点。在本研究中，设计并合成了一种用吡啶酰胺支架修饰的新型CXCR4抑制剂（CPZ1344）。然后评估其抗GBM功能。我们的结果表明，CPZ1344 以浓度依赖性方式减少 GBM 细胞的生长。 CPZ1344 的抗 GBM 活性是由于 GBM 细胞形态的改变和 GBM 细胞的凋亡诱导所致。 CPZ1344 抑制 U87 细胞的迁移和血管生成，导致细胞周期停滞在 G1 期并抑制 CXCR4 信号传导。这些发现证明了 CPZ1344 的抗癌作用及其作为新型抗 GBM 治疗药物的潜力。