Design and synthesis of new lenalidomide analogs via Suzuki cross-coupling reaction
文献类型：期刊论文
| 作者 | Xiao, Donghuai2; Wang, Yu-jie3; Wang, Han-lin1,3,4; Zhou, Yu-bo3 ; Li, Jia1,3,4,5; Lu, Wei2; Jin, Jiyu2
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| 刊名 | ARCHIV DER PHARMAZIE
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| 出版日期 | 2020-04-28 |
| 页码 | 10 |
| 关键词 | antitumor arylboronic acid lenalidomide Suzuki cross-coupling |
| ISSN号 | 0365-6233 |
| DOI | 10.1002/ardp.201900376 |
| 通讯作者 | Li, Jia(jli@simm.ac.cn) ; Lu, Wei(wlu@chem.ecnu.edu.cn) ; Jin, Jiyu(jyjin@chem.ecnu.edu.cn) |
| 英文摘要 | Lenalidomide is a cereblon modulator known for its antitumor, anti-inflammatory, and immunomodulatory properties in clinical applications. Recently, some reported lenalidomide analogs could exhibit a significant bioactivity through various modifications in the isoindolinone ring. In this study, we designed and synthesized a series of novel lenalidomide analogs on the basis of the installation of a methylene chain at the C-4 position of isoindolinone via the Suzuki cross-coupling reaction. These new compounds were further evaluated for their in vitro antiproliferative activities against two tumor cell lines (MM.1S and Mino). Specifically, compound 4c displayed the strongest antiproliferative activity against the MM.1S (IC50 = 0.27 +/- 0.03 mu M) and Mino (IC50 = 5.65 +/- 0.58 mu M) tumor cell lines. In summary, we have developed a new synthetic strategy for C-4 derivatization of lenalidomide, providing a bioactive scaffold that could be used to discover further potential antitumor lead compounds in pharmaceutical research. |
| WOS关键词 | THALIDOMIDE ANALOGS ; POTENT INHIBITORS ; CEREBLON ; DEGRADATION ; DEXAMETHASONE ; MODULATION ; ACTIVATION ; EFFICACY ; THERAPY ; TARGET |
| 资助项目 | National Natural Science Foundation of China[81125023] ; Shanghai Science and Technology Council[16DZ2280100] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000528856700001 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/280490]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Li, Jia; Lu, Wei; Jin, Jiyu |
| 作者单位 | 1.Shanghai Tech Univ, Sch Life Sci & Technol, Shanghai, Peoples R China 2.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China 3.Chinese Acad Sci, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, Beijing, Peoples R China 5.Pilot Natl Lab Marine Sci & Technol Qingdao, Open Studio Druggabil Res Marine Nat Prod Qingdao, Qingdao, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xiao, Donghuai,Wang, Yu-jie,Wang, Han-lin,et al. Design and synthesis of new lenalidomide analogs via Suzuki cross-coupling reaction[J]. ARCHIV DER PHARMAZIE,2020:10. |
| APA | Xiao, Donghuai.,Wang, Yu-jie.,Wang, Han-lin.,Zhou, Yu-bo.,Li, Jia.,...&Jin, Jiyu.(2020).Design and synthesis of new lenalidomide analogs via Suzuki cross-coupling reaction.ARCHIV DER PHARMAZIE,10. |
| MLA | Xiao, Donghuai,et al."Design and synthesis of new lenalidomide analogs via Suzuki cross-coupling reaction".ARCHIV DER PHARMAZIE (2020):10. |
入库方式： OAI收割
来源：上海药物研究所
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