2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin-2-ylthio) Acetamides as a New Class of Falcipain-2 Inhibitors. 3. Design, Synthesis and Biological Evaluation
文献类型：期刊论文
| 作者 | Zhu, Jin1; Chen, Tong1; Liu, Jie1; Ma, Ruoqun1; Lu, Weiqiang1; Huang, Jin1; Li, Honglin1; Li, Jian1; Jiang, Hualiang1,2
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| 刊名 | MOLECULES
 |
| 出版日期 | 2009-02 |
| 卷号 | 14期号:2页码:785-797 |
| 关键词 | 2-(3,4-Dihydro-4-oxothieno[2,3-d]pyrimidin-2-ylthio)acetamide derivatives Falcipain-2 inhibitor Malaria SAR |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules14020785 |
| 文献子类 | Article |
| 英文摘要 | The cysteine protease falcipain-2 (FP-2) of Plasmodium falciparum is a principal cysteine protease and an essential hemoglobinase of erythrocytic P. falciparum trophozoites, making it become an attractive target enzyme for developing anti-malarial drugs. In this study, a series of novel small molecule FP-2 inhibitors have been designed and synthesized based on compound 1, which was identified by using structure-based virtual screening in conjunction with an enzyme inhibition assay. All compounds showed high inhibitory effect against FP-2 with IC(50)s of 1.46-11.38 mu M, and the inhibitory activity of compound 2a was similar to 2 times greater than that of prototype compound 1. The preliminary SARs are summarized and should be helpful for future inhibitor design, and the novel scaffold presented here, with its potent inhibitory activity against FP-2, also has potential application in discovery of new anti-malarial drugs. |
| WOS关键词 | CYSTEINE PROTEASE INHIBITORS ; PLASMODIUM-FALCIPARUM ; RECOMBINANT FALCIPAIN-2 ; DERIVATIVES ; PROTEINASE ; IDENTIFICATION ; HEMOGLOBINASE ; RESISTANCE ; CRUZAIN |
| 资助项目 | National Natural Science Foundation of China[90813005] ; National Natural Science Foundation of China[30672539] ; National Natural Science Foundation of China[20803022] ; 863 Hi-Tech Program of China[2006AA020404] ; 863 Hi-Tech Program of China[2007AA02Z147] ; 863 Hi-Tech Program of China[2007AA02Z304] ; Shanghai Committee of Science and Technology[08JC1407800] ; Shanghai Ministry of Science and Technology[07QA14013] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000263823400015 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279335]  |
| 专题 | 药物发现与设计中心 |
| 通讯作者 | Huang, Jin |
| 作者单位 | 1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Jin,Chen, Tong,Liu, Jie,et al. 2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin-2-ylthio) Acetamides as a New Class of Falcipain-2 Inhibitors. 3. Design, Synthesis and Biological Evaluation[J]. MOLECULES,2009,14(2):785-797. |
| APA | Zhu, Jin.,Chen, Tong.,Liu, Jie.,Ma, Ruoqun.,Lu, Weiqiang.,...&Jiang, Hualiang.(2009).2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin-2-ylthio) Acetamides as a New Class of Falcipain-2 Inhibitors. 3. Design, Synthesis and Biological Evaluation.MOLECULES,14(2),785-797. |
| MLA | Zhu, Jin,et al."2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin-2-ylthio) Acetamides as a New Class of Falcipain-2 Inhibitors. 3. Design, Synthesis and Biological Evaluation".MOLECULES 14.2(2009):785-797. |
入库方式： OAI收割
来源：上海药物研究所
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