biostudies-literatureNiu JBOpen Fund of State Key Laboratory of Pharmaceutical Biotechnology, Nan-jing University, ChinaHenan Association of Science and TechnologyNational Natural Sciences Foundations of ChinaKey Laboratory of Biomedical Effects of Nanomaterials and Nanosafety, CASScience and Technology Department of Henan ProvinceChina Postdoctoral Science FoundationMedical Science and Technology Project of Henan Province1715-1731https://www.ebi.ac.uk/biostudies/studies/S-EPMC8386742biostudies-literatureUnknown36(1)Hippo signalling pathway plays a crucial role in tumorigenesis and cancer progression. In this work, we identified an <i>N-aryl sulphonamide-quinazoline derivative</i>, compound <b>9i</b> as an anti-gastric cancer agent, which exhibited potent antiproliferative ability with IC₅₀ values of 0.36 μM (MGC-803 cells), 0.70 μM (HCT-116 cells), 1.04 μM (PC-3 cells), and 0.81 μM (MCF-7 cells), respectively and inhibited YAP activity by the activation of p-LATS. Compound <b>9i</b> was effective in suppressing MGC-803 xenograft tumour growth in nude mice without obvious toxicity and significantly down-regulated the expression of YAP <i>in vivo</i>. Compound <b>9i</b> arrested cells in the G2/M phase, induced intrinsic apoptosis, and inhibited cell colony formation in MGC-803 and SGC-7901 Journal of enzyme inhibition and medicinal chemistryDiscovery of <i>N</i>-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents <i>in vitro</i> and <i>in vivo via</i> activating the Hippo signalling pathway.PMC8386742320009982020HYTP056NSKF202011KF-GN-202101LHGJ202004452018M63281220202310144U2004123816733222019TQ02852019M662513Hua CQLiu YYang JJLi YRQi YQJin CYZhang YBNiu JBYu GXSong JZhang SYfalseDiscovery of <i>N</i>-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents <i>in vitro</i> and <i>in vivo via</i> activating the Hippo signalling pathway.Hippo signalling pathway plays a crucial role in tumorigenesis and cancer progression. In this work, we identified an <i>N-aryl sulphonamide-quinazoline derivative</i>, compound <b>9i</b> as an anti-gastric cancer agent, which exhibited potent antiproliferative ability with IC₅₀ values of 0.36 μM (MGC-803 cells), 0.70 μM (HCT-116 cells), 1.04 μM (PC-3 cells), and 0.81 μM (MCF-7 cells), respectively and inhibited YAP activity by the activation of p-LATS. Compound <b>9i</b> was effective in suppressing MGC-803 xenograft tumour growth in nude mice without obvious toxicity and significantly down-regulated the expression of YAP <i>in vivo</i>. Compound <b>9i</b> arrested cells in the G2/M phase, induced intrinsic apoptosis, and inhibited cell colony formation in MGC-803 and SGC-7901 2021-01-01T00:00:00Z2021 Dec2026-05-08T18:15:30.259Z2022-02-11T09:46:29.259ZS-EPMC83867423442571610.1080/14756366.2021.1958211