{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Niu JB"],"funding":["Open Fund of State Key Laboratory of Pharmaceutical Biotechnology, Nan-jing University, China","Henan Association of Science and Technology","National Natural Sciences Foundations of China","Key Laboratory of Biomedical Effects of Nanomaterials and Nanosafety, CAS","Science and Technology Department of Henan Province","China Postdoctoral Science Foundation","Medical Science and Technology Project of Henan Province"],"pagination":["1715-1731"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8386742"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["36(1)"],"pubmed_abstract":["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 IC<sub>50</sub> 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":["Journal of enzyme inhibition and medicinal chemistry"],"pubmed_title":["Discovery 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."],"pmcid":["PMC8386742"],"funding_grant_id":["32000998","2020HYTP056","NSKF202011","KF-GN-202101","LHGJ20200445","2018M632812","20202310144","U2004123","81673322","2019TQ0285","2019M662513"],"pubmed_authors":["Hua CQ","Liu Y","Yang JJ","Li YR","Qi YQ","Jin CY","Zhang YB","Niu JB","Yu GX","Song J","Zhang SY"],"additional_accession":[]},"is_claimable":false,"name":"Discovery 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.","description":"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 IC<sub>50</sub> 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 ","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Dec","modification":"2026-05-08T18:15:30.259Z","creation":"2022-02-11T09:46:29.259Z"},"accession":"S-EPMC8386742","cross_references":{"pubmed":["34425716"],"doi":["10.1080/14756366.2021.1958211"]}}