Discovery of N-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents in vitro and in vivo via activating the Hippo signalling pathway
Hippo signalling pathway plays a crucial role in tumorigenesis and cancer progression. In this work, we identified an N-aryl sulphonamide-quinazoline derivative, compound 9i as an anti-gastric cancer agent, which exhibited potent antiproliferative ability with IC50 values of 0.36 μM (MGC-803 cells),...
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Taylor & Francis Group,
2021-01-01T00:00:00Z.
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| 001 | doaj_8ef17c5ecd874c5ebebd48e3d50c3f93 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Jin-Bo Niu |e author |
| 700 | 1 | 0 | |a Chun-Hua Quan |e author |
| 700 | 1 | 0 | |a Yuan Liu |e author |
| 700 | 1 | 0 | |a Guang-Xi Yu |e author |
| 700 | 1 | 0 | |a Jia-Jia Yang |e author |
| 700 | 1 | 0 | |a Yin-Ru Li |e author |
| 700 | 1 | 0 | |a Yan-Bing Zhang |e author |
| 700 | 1 | 0 | |a Ying-Qiu Qi |e author |
| 700 | 1 | 0 | |a Jian Song |e author |
| 700 | 1 | 0 | |a Cheng-Yun Jin |e author |
| 700 | 1 | 0 | |a Sai-Yang Zhang |e author |
| 245 | 0 | 0 | |a Discovery of N-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents in vitro and in vivo via activating the Hippo signalling pathway |
| 260 | |b Taylor & Francis Group, |c 2021-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2021.1958211 | ||
| 520 | |a Hippo signalling pathway plays a crucial role in tumorigenesis and cancer progression. In this work, we identified an N-aryl sulphonamide-quinazoline derivative, compound 9i 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 9i was effective in suppressing MGC-803 xenograft tumour growth in nude mice without obvious toxicity and significantly down-regulated the expression of YAP in vivo. Compound 9i arrested cells in the G2/M phase, induced intrinsic apoptosis, and inhibited cell colony formation in MGC-803 and SGC-7901 cells. Therefore, compound 9i is to be reported as an anti-gastric cancer agent via activating the Hippo signalling pathway and might help foster a new strategy for the cancer treatment by activating the Hippo signalling pathway regulatory function to inhibit the activity of YAP. | ||
| 546 | |a EN | ||
| 690 | |a hippo signalling pathway | ||
| 690 | |a yap | ||
| 690 | |a n-aryl sulphonamide-quinazoline | ||
| 690 | |a anti-proliferative activity | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1715-1731 (2021) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2021.1958211 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/8ef17c5ecd874c5ebebd48e3d50c3f93 |z Connect to this object online. |