CAS: 118409-62-4; 2-(3-Hydroxy-4-Nitrobenzylidene)Malononitrile

上下游产品

5-formyl-2-nitrophenol malononitrile

📜3-羟基-4-硝基苯甲醛,丙二腈置于哌啶体系中,用 乙醇 用作溶剂,以78%的收率获得酪氨酸磷酸化抑制剂126
参考文献:Tyrphostins I: Synthesis And Biological Activity Of Protein Tyrosine Kinase Inhibitors
标题:Tyrphostins I: Synthesis And Biological Activity Of Protein Tyrosine Kinase Inhibitors
摘要:A Novel Class Of Low Molecular Weight Protein Tyrosine Kinase Inhibitors Is Described. These Compounds Constitute A Systematic Series Of Molecules With A Progressive Increase In Affinity Toward The Substrate Site Of The Egf Receptor Kinase Domain. These Competitive Inhibitors Also Effectively Block The Egf-Dependent Autophosphorylation Of The Receptor. The Potent Egf Receptor Kinase Blockers Examined Were Found To Competitively Inhibit The Homologous Insulin Receptor Kinase At 10(2)-10(3) Higher Inhibitor Concentrations In Spite Of The Significant Homology Between These Protein Tyrosine Kinases. These Results Demonstrate The Ability To Synthesize Selective Tyrosine Kinase Inhibitors. The Most Potent Egf Receptor Kinase Inhibitors Also Inhibit The Egf-Dependent Proliferation Of A431/clone 15 Cells With Little Or No Effect On Egf Independent Cell Growth. These Results Demonstrate The Potential Use Of Protein Tyrosine Kinase Inhibitors As Selective Antiproliferative Agents For Proliferative Diseases Caused By The Hyperactivity Of Protein Tyrosine Kinases. We Have Suggested The Name "Tyrphostins" For This Class Of Antiproliferative Compounds Which Act As Protein Tyrosine Kinase Blockers.
Doi:10.1021/jm00130A020

专利信息

专利号:WO-2024213057-A1
优先权日:2023-04-12
标题:Use of combination of lsd1 inhibitor and drug to treat cancer
发明人：LIU HONG; LI JIA; HUANG HE; WANG JIANG; ZHOU YUBO; REN XUELIAN; LI CHUNPU; KAN WEIJUAN; XU ZICHAO; HU XIAOBEI; WU HENGBO; WANG HANLIN; YE YUNFEI; QIU XIAOHUI; SU MINGBO
权利人:SHANGHAI INST MATERIA MEDICA CAS
摘要:A use of a combination of an LSD1 inhibitor and a drug to treat cancer. Specifically, provided is a composition comprising: a tranylcypromine compound and/or a derivative thereof; and a drug selected from a kinase inhibitor, an anti-cancer drug acting upon or affecting the DNA, an antiviral compound, an antihypertension compound, an antidiabetic compound, a JAK-STAT signaling pathway inhibitor, an NF-κB signaling pathway inhibitor, a protein synthesis inhibitor, a 5-hydroxytryptamine receptor agonist, a dystroglycan modulator, a GABA receptor modulator, or a combination thereof. The two active ingredients have a synergistic effect, and the synergistic treatment effect is significantly better than that of the two individually, thereby remarkably improving the cancer treatment effect.

专利号:US-7052692-B1
优先权日:1997-09-02
标题:Role of tyrosine phosphorylation of a cellular protein in adeno-associated virus 2-mediated transgene expression
发明人：SRIVASTAVA ARUN; QING KEYUN; WANG XU-SHAN; PONNAZHAGAN SELVARANGAN; BAJPAI ANIL
权利人:ADVANCED RES & TECH INST
摘要:The present invention identifies a protein, designated the D-sequence-binding protein (D-BP), is phosphorylated at tyrosine residues and blocks AAV-mediated transgene expression in infected cells by inhibiting the leading strand viral DNA synthesis. More particularly, the present invention demonstrates that D-BP is phosphorylated by EGF-R protein tyrosine kinase. Methods of increasing transcription and promoting replication of transgenes exploiting this information are disclosed herein.