A novel derivative of quinazoline, WYK431 induces G2/M phase arrest and apoptosis in human gastric cancer BGC823 cells through the PI3K/Akt pathway.

摘要: WYK431, a novel synthetic quinazoline derivative, showing potent inhibition of proliferation activity against broad spectrum human cancer cell lines. We investigated the anticancer effects WYK431 on BGC823 cells both in vitro and vivo. The results showed that inhibited proliferation, arrested cycle at G(2)/M phase, which was related to CDK1 CDC25C, induced apoptosis associated with activation caspase-3 caspase-9 rather than caspase-8 cells. Treatment resulted upregulation Bax, release cytochrome c from mitochondria cytosol disruption mitochondrial membrane potential. Western blot analysis downregulated levels PI3K/Akt signaling pathway. Moreover, effectively suppressed tumor growth xenograft models BALB/c athymic nude mice without major side action. TUNEL Collectively, is small molecule agent inhibits inducing phase arrest via apoptotic To assess its potential as promising requires further investigation.