CAS: 882257-11-6; 1-(5-((2,3-Dichlorophenyl)Thio)-4-Nitrothiophen-2-yl)Ethan-1-One

上下游产品

5-acetyl-2-chloro-3-nitrothiophene 2,3-dichlorobenzenethiol 2-acetyl-5-chlorothiophene1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitro-2-thienyl]ethanol

📜2-乙酰基-5-氯噻酚置于硝酸,Sodium Methylate体系中,用 甲醇 作为反应溶剂,化学反应 1.75H,反应生成 1-[5-[(2,3-二氯苯基)硫基]-4-硝基-2-噻吩基]-乙酮
参考文献:Selective Dual Inhibitors Of The Cancer-Related Deubiquitylating Proteases Usp7 And Usp47
标题:Selective Dual Inhibitors Of The Cancer-Related Deubiquitylating Proteases Usp7 And Usp47
摘要:Inhibitors Of The Cancer-Related Cysteine Isopeptidase Human Ubiquitin-Specific Proteases 7 (Usp7) And 47 (Usp47) Are Considered To Have Potential As Cancer Therapeutics,Owing To Their Ability To Stabilize The Tumor Suppressor P53 And To Decrease Dna Polymerase Beta (Pol Beta),Both Of Which Are Potential Anticancer Effects. A New Class Of Dual Small Molecule Inhibitors Of These Enzymes Has Been Discovered. Compound 1,A Selective Inhibitor Of Usp7 And Usp47 With Moderate Potency,Demonstrates Inhibition Of Usp7 In Cells And Induces Elevated P53 And Apoptosis In Cancer Cell Lines. Compound 1 Has Been Shown To Demonstrate Modest Activity In Human Xenograft Multiple Myeloma And B-Cell Leukemia In Vivo Models. This Activity May Be The Result Of Dual Inhibition Of Usp7 And Usp47. To Address Issues Regarding Potency And Developability,Analogues Of Compound 1 Have Been Synthesized And Tested,Leading To Improvements In Potency,Solubility,And Metabolic Reactivity Profile. Further Optimization Is Expected To Yield Preclinical Candidates And,Ultimately,Clinical Candidates For The Treatment Of Multiple Myeloma,Prostate Cancer,And Other Cancers.
DOI:10.1021/ml200276J