412339-20-9Relevant academic research and scientific papers
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
, (2021/09/20)
Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
4-phenoxy pyridine derivative containing 3-pyridazinone structure, 4-pyridazinone structure and 1,2,4-triazinone structure, and applications thereof.
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Paragraph 0062; 0074-0075, (2020/02/04)
The invention relates to a 4-phenoxy pyridine derivative containing a 3-pyridazinone structure, a 4-pyridazinone structure and a 1,2,4-triazinone structure, and applications thereof. According to theinvention, the 4-phenoxy pyridine derivative has a struc
Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors
Chen, Ye,Ding, Shi,Gong, Yilin,Hao, Xuechen,Hou, Yunlei,Liu, Ju,Liu, Yajing,Shi, Jiantao,Wang, Yang,Zhou, Yunpeng
, (2020/03/31)
Three series of novel 4-phenoxypyridine derivatives containing 4-methyl-6-oxo-1,6-dihydropyridazine- 3-carboxamide, 5-methyl-4-oxo-1,4-dihydropyridazine-3-carboxamide and 4-methyl-3,5-dioxo-2,3,4,5- tetrahydro-1,2,4-triazine-6-carboxamide moieties were synthesized and evaluated for their in vitro inhibitory activitives against c-Met kinase and cytotoxic activitives against A549, H460, HT-29 cancer cell lines. The results indicated that most of the compounds showed moderate to good antitumor activitives. The most promising compound 26a (with c-Met IC50 value of 0.016 μM) showed remarkable cytotoxicity against A549, H460, and HT-29 cell lines with IC50 values of 1.59 μM, 0.72 μM and 0.56 μM, respectively. Their preliminary structure-activity relationships (SARs) studies indicate that 4-methyl-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carboxamide was more preferred as linker part, and electron-withdrawing groups on the terminal phenyl rings are beneficial for improving the antitumor activitives. Furthermore, the colony formation, acridine orange/ethidium bromide (AO/EB) staining, apoptosis, and wound-healing assay of 26a were performed on HT-29 and/or A549 cell lines.
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment
Duan, Yongli,Tang, Qidong,Xiong, Hehua,Zhang, Han,Zhang, Jianqing,Zhang, Qian,Zheng, Pengwu
, (2020/03/23)
A series of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment were designed, synthesized, and evaluated for their biological activity. Most compounds showed effective inhibitory activity against cancer cell lines of A
Dihydropyridine structure contained 7-nitrogenous indoles compound and application thereof
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, (2017/08/02)
The invention discloses a dihydropyridine structure contained 7-nitrogenous indoles compound and geometrical isomer, pharmacologically acceptable salt, hydrate, solvate or prodrug and preparation method thereof. The dihydropyridine structure contained 7-nitrogenous indoles compound and the pharmacologically acceptable salt, hydrate or solvate serve as activities and are mixed and prepared into the compound with a pharmacologically acceptable carrier or a polybutene, and the clinically acceptable dosage form is prepared. The dihydropyridine structure contained 7-nitrogenous indoles compound is applied to preparation of disease drugs in treatment and/or prevention of hyperplastic disease, cancer and lung cancer, liver cancer, stomach cancer, colon cancer and breast cancer.
Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors
Tang, Qidong,Wang, Linxiao,Duan, Yongli,Wang, Wenhui,Huang, Shunmin,Zhi, Jia,Jia, Shuang,Zhu, Wufu,Wang, Ping,Luo, Rong,Zheng, Pengwu
, p. 97 - 106 (2017/04/07)
A series of 7-azaindole derivatives bearing the dihydropyridazine scaffold were synthesized and evaluated for their c-Met kinase inhibitory, and antiproliferative activity against 4 cancer cell lines (HT29, A549, H460, U87MG) were evaluated in?vitro. Most compounds showed moderate to excellent potency. Compared to foretinib, the most promising analog 34 (c-Met IC50: 1.06?nM, a multitarget tyrosine kinase inhibitor) showed a 6.4-, 7.8-, and 3.2-fold increase in activity against HT29, A549, and H460?cell lines, respectively. Structure activity relationship studies indicated that mono-EWGs (such as R2?=?F) at 4-position of moiety D was a key factor in improving the antitumor activity.
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents
Zhou, Shunguang,Liao, Huimin,He, Chao,Dou, Yanan,Jiang, Mingyan,Ren, Lixiang,Zhao, Yanfang,Gong, Ping
, p. 581 - 593 (2014/07/21)
A series of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety were synthesized and evaluated for their in vitro cytotoxic activity against five cancer cell lines (HT-29, H460, A549, MKN-45, and U87MG). Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines. Compounds 15a, 20a, 15b, 15c, 20d, and 16e were further examined for their inhibitory activity against c-Met kinase. The most promising compound 15a (c-Met half-maximal inhibitory concentration [IC50] = 2.15 nM) showed remarkable cytotoxicity against HT-29, H460, and A549 cell lines with IC50 values of 0.10 μM, 0.13 μM, and 0.05 μM, respectively, and thus it was 1.5- to 2.3-fold more potent than foretinib. Their preliminary structure-activity relationships (SARs) studies indicate that electron-withdrawing groups on the terminal phenyl rings are beneficial for improving the antitumor activity.
