5氨基吡唑及5氨基三唑类成纤维细胞生长因子受体激酶抑制剂的设计合成
文献类型：期刊论文
| 作者 | 董潜1; 彭霞2; 王雯1; 戴阳2; 赵伟利1; 艾菁2 ; 董肖椿1
|
| 刊名 | 有机化学
 |
| 出版日期 | 2015 |
| 卷号 | 35期号:9页码:1939 |
| 关键词 | SELECTIVE INHIBITOR ACTIVATING MUTATIONS TYROSINE KINASE CANCER POTENT CARCINOMA FAMILY FGFR2 5-aminopyrazole 5-amino-1,2,3-triazole FGFR inhibitors anti-tumor agent |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201503045 |
| 英文摘要 | Fibroblast growth factor receptor (FGFR) is a promising therapeutic target for cancer treatment. A series of 5-aminopyrazole and 5-amino-1,2,3-triazole derivatives were designed as FGFR inhibitors based on the docking mode of Debio1347 within the FGFR kinase domain. The inhibitory effects on FGFR2 kinase and the antitumor activities against human gastric cancer SNU16 cell lines were evaluated. Furthermore, the preliminary structure-activity relationships (SAR) was discussed. The results demonstrated that several compounds present good potency against FGFR2 kinase. (2-methyl-1H-benzo dimidazol-6-yl)-1H-pyrazol-4-yl)-1-(1H-thieno3,2-bpyrrol-2-yOmethanone (8) and 1-(5-amino-1-(2-methyl-1H-benzodimidazol-6-yl)-1H-1,2,3-triazol-4-yl)-1-(1H-indol-2-yl)methanone (18) were the most potent with 1050 values of 3.3 and 2.3 nmol.L-1, respectively, which are similar to that of Debio1347. Compounds 8 and 18 exhibited slightly weaker antitumor activity against SNU16 cell lines than Debio1347 with IC50 value of 77.3, 155.2 nmol.L-1, respectively. |
| 资助项目 | [Specialized Research Fund for the Doctoral Program of Higher Education of China] ; [Shanghai Municipal Science & Technology Pillar Program for Bio-pharmaceuticals] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/287968]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.复旦大学 2.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | 董潜,彭霞,王雯,等. 5氨基吡唑及5氨基三唑类成纤维细胞生长因子受体激酶抑制剂的设计合成[J]. 有机化学,2015,35(9):1939. |
| APA | 董潜.,彭霞.,王雯.,戴阳.,赵伟利.,...&董肖椿.(2015).5氨基吡唑及5氨基三唑类成纤维细胞生长因子受体激酶抑制剂的设计合成.有机化学,35(9),1939. |
| MLA | 董潜,et al."5氨基吡唑及5氨基三唑类成纤维细胞生长因子受体激酶抑制剂的设计合成".有机化学 35.9(2015):1939. |
入库方式： OAI收割
来源：上海药物研究所
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