CAS: 1020149-73-8; N-(4-((2-Amino-6-Methylpyrimidin-4-yl)Amino)Phenyl)-4-(Quinolin-4-Ylamino)Benzamide

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N-[4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl]-4-nitrobenzamide 4-chloroquinoline 2-amino-6-methyl-4-chloropyrimidine p-aminoethylbenzoate

📜4-氯喹啉置于盐酸,Benzotriazol-1-Yloxyl-Tris-(Pyrrolidino)-Phosphonium Hexafluorophosphate,三乙胺,Potassium Hydroxide体系中,用 乙醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 2.5H,反应生成N-[4-[(2-氨基-6-甲基-4-嘧啶基)氨基]苯基]-4-(4-喹啉基氨基)苯甲酰胺
参考文献:Selective Non-Nucleoside Inhibitors Of Human Dna Methyltransferases Active In Cancer Including In Cancer Stem Cells
标题:Selective Non-Nucleoside Inhibitors Of Human Dna Methyltransferases Active In Cancer Including In Cancer Stem Cells
摘要:Dna Methyltransferases (Dnmts) Are Important Enzymes Involved In Epigenetic Control Of Gene Expression And Represent Valuable Targets In Cancer Chemotherapy. A Number Of Nucleoside Dnmt Inhibitors (Dnmti) Have Been Studied In Cancer,Including In Cancer Stem Cells,And Two Of Them (Azacytidine And Decitabine) Have Been Approved For Treatment Of Myelodysplastic Syndromes. However,Only A Few Non-Nucleoside Dnmti Have Been Identified So Far,And Even Fewer Have Been Validated In Cancer. Through A Process Of Hit-To-Lead Optimization,We Report Here The Discovery Of Compound 5 As A Potent Non-Nucleoside Dnmti That Is Also Selective Toward Other Ado Met-Dependent Protein Methyltransferases. Compound 5 Was Potent At Single-Digit Micromolar Concentrations Against A Panel Of Cancer Cells And Was Less Toxic In Peripheral Blood Mononuclear Cells Than Two Other Compounds Tested. In Mouse Medulloblastoma Stem Cells,5 Inhibited Cell Growth,Whereas Related Compound 2 Showed High Cell Differentiation. To The Best Of Our Knowledge,2 And 5 Are The First Non-Nucleoside Dnmti Tested In A Cancer Stem Cell Line.
Doi:10.1021/jm4012627

专利信息

专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人：SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.

专利号:US-11674950-B2
优先权日:2017-10-31
标题 :Methods determining and treating cellular resistance to ADP-rtbosylating toxin
发明人：LANE ANDREW; ASTER JON
权利人:DANA FARBER CANCER INST INC; BRIGHAM & WOMENS HOSPITAL INC
摘要:The present invention is based in part on the identification of DPH1 and other members of the diphthamide synthesis pathway as biomarkers of resistance to an ADP-ribosylating toxin in a cell, and methods for identification, assessment, and treatment of a condition that is resistant to an ADP-ribosylating toxin.