Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors
文献类型：期刊论文
| 作者 | Yang, Wei1; Li, Lixuan2,3; Ji, Xun1; Wu, Xiaowei1; Su, Mingbo3; Sheng, Li3; Zang, Yi3 ; Li, Jia2,3; Liu, Hong1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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| 出版日期 | 2014-11-01 |
| 卷号 | 22期号:21页码:6146-6155 |
| 关键词 | HDACs HDACs inhibitor Hydroxamic acid Thieno[2,3-d]pyrimidines |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2014.08.030 |
| 文献子类 | Article |
| 英文摘要 | A series of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel HDACs inhibitors were designed, synthesized and evaluated. Most of these compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10r against HDAC1, HDAC3, HDAC6 was 1.14 +/- 0.03 nM, 3.56 +/- 0.08 nM, 11.43 +/- 0.12 nM. Compound 10r noticeably up-regulated the level of histone H3 acetylation compared to the SAHA. Most of the compounds showed the strong anti-proliferative activity against human cancer cell lines including RMPI8226 and HCT-116. The IC50 values of Compounds 10r and 10t against RPMI8226 was 2.39 +/- 0.20 mu M, 1.41 +/- 0.44 mu M, respectively, and the HCT-116 was sensitive to the compounds 10h, 10m, 10r, 10w with the IC50 values < 1.9 mu M. (C) 2014 Elsevier Ltd. All rights reserved. |
| WOS关键词 | DUAL EGFR/ERBB-2 INHIBITORS ; PROSTATE-CANCER ; HDAC INHIBITORS ; ANTIMALARIAL THERAPY ; KINASE INHIBITORS ; SOLID TUMORS ; IN-VIVO ; TRANSCRIPTION ; DEPSIPEPTIDE ; EXPRESSION |
| 资助项目 | National Natural Science Foundation of China[21021063] ; National Natural Science Foundation of China[91229204] ; National Natural Science Foundation of China[81125023] ; National Natural Science Foundation of China[81173033] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103101-072] ; National S&T Major Projects[2012ZX09301001-005] ; National S&T Major Projects[2013ZX09507-001] ; Chinese Academy of Science[XDA01040303] ; Program of Shanghai Subject Chief Scientist[12XD1407100] ; Program of Shanghai Subject Chief Scientist[13XD1404300] ; National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program' of China[2014ZX09507-002] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000344471800043 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276853]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 2.E China Normal Univ, Inst Adv Interdisciplinary Res, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, SIBS, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Wei,Li, Lixuan,Ji, Xun,et al. Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2014,22(21):6146-6155. |
| APA | Yang, Wei.,Li, Lixuan.,Ji, Xun.,Wu, Xiaowei.,Su, Mingbo.,...&Liu, Hong.(2014).Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,22(21),6146-6155. |
| MLA | Yang, Wei,et al."Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 22.21(2014):6146-6155. |
入库方式： OAI收割
来源：上海药物研究所
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