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Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma

文献类型：期刊论文

作者Liu, Zhihao5; Lin, Min5; Liu, Chenyu4; Chen, Xin5; Chen, Qian5; Li, Xinyu3; Wu, Xiaoyan3; Wang, Yahui2; Wang, Lei5; Yang, Fan4
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2024-04-04
页码14
ISSN号0022-2623
DOI10.1021/acs.jmedchem.3c02265
通讯作者Jin, Jia(aukaukauk@163.com) ; Ye, Fei(yefei@zstu.edu.cn)
英文摘要Coactivator-associated arginine methyltransferase 1 (CARM1), an important member of type I protein arginine methyltransferases (PRMTs), has emerged as a promising therapeutic target for various cancer types. In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (6) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. In this work, we conducted chemical modifications on compound 6, resulting in a series of (2-(benzyloxy)phenyl)methanamine derivatives as potent inhibitors of CARM1. Among them, compound 17e displayed remarkable potency and selectivity for CARM1 (IC50 = 2 +/- 1 nM), along with notable antiproliferative effects against melanoma cell lines. Cellular thermal shift assay and western blot experiments confirmed that compound 6 effectively targets CARM1 within cells. Furthermore, compound 17e displayed good antitumor efficacy in a melanoma xenograft model, indicating that this compound warrants further investigation as a potential anticancer agent.
WOS关键词ARGININE METHYLTRANSFERASE 1 ; METHYLATION ; TUMOR ; AMBER
资助项目National Natural Science Foundation of China[82373729] ; National Natural Science Foundation of China[81803339] ; National Natural Science Foundation of China[LY23H300004] ; Zhejiang Province Natural Science Foundation[22042292-Y] ; Zhejiang Province Natural Science Foundation[23042124-Y] ; Fundamental Research Funds of Zhejiang Sci-Tech University
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001197309700001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/310789]  
专题新药研究国家重点实验室
通讯作者Jin, Jia; Ye, Fei
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Bengbu Med Coll, Affiliated Hosp 1, Dept Anesthesiol, Bengbu City 233000, Peoples R China
3.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310000, Peoples R China
4.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug Dev, Shanghai 200062, Peoples R China
5.Zhejiang Sci Tech Univ, Coll Life Sci & Med, Hangzhou 310018, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Zhihao,Lin, Min,Liu, Chenyu,et al. Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma[J]. JOURNAL OF MEDICINAL CHEMISTRY,2024:14.
APA Liu, Zhihao.,Lin, Min.,Liu, Chenyu.,Chen, Xin.,Chen, Qian.,...&Ye, Fei.(2024).Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.JOURNAL OF MEDICINAL CHEMISTRY,14.
MLA Liu, Zhihao,et al."Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma".JOURNAL OF MEDICINAL CHEMISTRY (2024):14.

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来源：上海药物研究所

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