An article Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia WOS:000471834500012 published article about ANDROGEN RECEPTOR; HISTONE H3; COACTIVATOR; CARM1; METHYLATION; DISCOVERY; TRANSCRIPTION; EXPRESSION in [Guo, Zuhao; Cao, Danyan; Chen, Danqi; Wang, Qi; Li, Yanlian; Li, Jian; Du, Zhiyan; Wang, Xin; Chen, Lin; Shen, Jingkang; Xiong, Bing] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Zhang, Zhuqing; Yang, Hong; Xu, Xiaowei; Zheng, Xineng; Ding, Jian; Geng, Meiyu; Huang, Xun] Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Zhang, Zhuqing; Xu, Xiaowei; Zheng, Xineng; Wang, Qi; Ding, Jian; Geng, Meiyu; Huang, Xun; Xiong, Bing] Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China in 2019.0, Cited 46.0. SDS of cas: 64-10-8. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8
PRMT4 is a type I protein arginine methyltransferase and plays important roles in various cellular processes. Overexpression of PRMT4 has been found to be involved in several types of cancers. Selective and in vivo effective PRMT4 inhibitors are needed for demonstrating PRMT4 as a promising therapeutic target. On the basis of compound 6, a weak dual PRMT4/6 inhibitor, we constructed a tetrahydroisoquinoline scaffold through a cut-and-sew scaffold hopping strategy. The subsequent SAR optimization efforts employed structure-based approach led to the identification of a novel PRMT4 inhibitor 49. Compound 49 exhibited prominently high potency and selectivity, moderate pharmacokinetic profiles, and good antitumor efficacy in acute myeloid leukemia xenograft model via oral administration, thus demonstrating this compound as a useful pharmacological tool for further target validation and drug development in cancer therapy.
SDS of cas: 64-10-8. About 1-Phenylurea, If you have any questions, you can contact Guo, ZH; Zhang, ZQ; Yang, H; Cao, DY; Xu, XW; Zheng, XN; Chen, DQ; Wang, Q; Li, YL; Li, J; Du, ZY; Wang, X; Chen, L; Ding, J; Shen, JK; Geng, MY; Huang, X; Xiong, B or concate me.
Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem