Novel Potent Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitors: Synthesis, Structure-Activity Relationships, and Antitumor Activities of 2-Indolinone Derivatives
文献类型：期刊论文
| 作者 | Cho, Tang Peng2; Dong, Su Yi1; Jun, Feng; Hong, Fu Jian2; Liang, Yang Jiang2; Lu, Xiao2; Hua, Peng Jiang2; Li, Li Ya2; Lei, Zhang2; Bing, Hu2 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2010-11-25 |
| 卷号 | 53期号:22页码:8140-8149 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/jm101036c |
| 文献子类 | Article |
| 英文摘要 | The inhibition of receptor tyrosine kinases (RTKs) has become a successful approach in the development of anticancer agents. Many potent small-molecule kinase inhibitors have been discovered. We report herein a series of pyrrolo-fused-heterocycle-2-indolinone analogues as inhibitors of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR). and c-Kit. Among them, some pyrrolo-fused six- and seven-membered-heterocycle derivatives such as 9, 15, 23, and 25 are potent inhibitors of VEGFR, PDGFR, and c-Kit both enzymatically ( < 50 nM) and cellularly, ( < 50 nM). Furthermore, compounds 9 and 25 possess favorable pharmacokinetic profiles and demonstrate good efficacies against human HT-29 cell colon tumor xenografts in nude mice. Further evaluations are in progress. |
| WOS关键词 | ANGIOGENESIS ; DISCOVERY |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:000284287200023 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278714]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Jun, Feng |
| 作者单位 | 1.Shanghai Chemikine Co Ltd, Shanghai, Peoples R China; 2.Shanghai Hengrui Pharmaceut Co Ltd, Shanghai 200245, Peoples R China; 3.Shanghai Inst Mat Med, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cho, Tang Peng,Dong, Su Yi,Jun, Feng,et al. Novel Potent Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitors: Synthesis, Structure-Activity Relationships, and Antitumor Activities of 2-Indolinone Derivatives[J]. JOURNAL OF MEDICINAL CHEMISTRY,2010,53(22):8140-8149. |
| APA | Cho, Tang Peng.,Dong, Su Yi.,Jun, Feng.,Hong, Fu Jian.,Liang, Yang Jiang.,...&Tai, Mong Xian.(2010).Novel Potent Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitors: Synthesis, Structure-Activity Relationships, and Antitumor Activities of 2-Indolinone Derivatives.JOURNAL OF MEDICINAL CHEMISTRY,53(22),8140-8149. |
| MLA | Cho, Tang Peng,et al."Novel Potent Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitors: Synthesis, Structure-Activity Relationships, and Antitumor Activities of 2-Indolinone Derivatives".JOURNAL OF MEDICINAL CHEMISTRY 53.22(2010):8140-8149. |
入库方式： OAI收割
来源：上海药物研究所
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