CAS: 5335-29-5; 3-Chloro-4-Phenoxyaniline

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CAS号56966-69-9 Benzene,2-chlor... | CAS号350-30-1 3-氯-4-氟硝基苯 | CAS号7439-89-6 铁粉 | CAS号108-95-2 苯酚 | CAS号29682-39-1 1-溴-2-氯-4-硝基苯 | CAS号56966-69-9 Benzene,2-chlor...

📜1-溴-2-氯-4-硝基苯置于caesium Carbonate,Tin(Ll) Chloride体系中,用 乙醇,甲苯 作为反应溶剂,化学反应生成 3-氯-4-苯氧基苯胺
参考文献:Discovery And Structure-activity Relationships Of Modified Salicylanilides As Cell Permeable Inhibitors Of Poly(Adp-Ribose) Glycohydrolase (Parg)
标题:Discovery And Structure-activity Relationships Of Modified Salicylanilides As Cell Permeable Inhibitors Of Poly(Adp-Ribose) Glycohydrolase (Parg)
摘要:The Metabolism Of Poly(Adp-Ribose) (Par) In Response To Dna Strand Breaks,Which Involves The Concerted Activities Of Poly(Adp-Ribose) Polymerases (Parps) And Poly(Adp-Ribose) Glycohydrolase (Parg),Modulates Cell Recovery Or Cell Death Depending Upon The Level Of Dna Damage. While Parp Inhibitors Show High Promise In Clinical Trials Because Of Their Low Toxicity And Selectivity For Brca Related Cancers,Evaluation Of The Therapeutic Potential Of Parg Is Limited By The Lack Of Well-Validated Cell Permeable Inhibitors. In This Study,Target-Related Affinity Profiling (Trap),An Alternative To High-Throughput Screening,Was Used To Identify A Number Of Druglike Compounds From Several Chemical Classes That Demonstrated Parg Inhibition In The Low-Micromolar Range. A Number Of Analogues Of One Of The Most Active Chemotypes Were Synthesized To Explore The Structure Activity Relationship (Sar) For That Series. This Led To The Discovery Of A Putative Pharmacophore For Parg Inhibition That Contains A Modified Salicylanilide Structure. Interestingly,These Compounds Also Inhibit Parp-1,Indicating Strong Homology In The Active Sites Of Parg And Parp-1 And Raising A New Challenge For Development Of Parg Specific Inhibitors. The Cellular Activity Of A Lead Inhibitor Was Demonstrated By The Inhibition Of Both Parp And Parg Activity In Squamous Cell Carcinoma Cells,Although Preferential Inhibition Of Parg Relative To Parp Was Observed. The Ability Of Inhibitors To Modulate Par Metabolism Via Simultaneous Effects On Parps And Parg May Represent A New Approach For Therapeutic Development.
DOI:10.1021/jm200325S

专利信息

专利号:US-7579356-B2
优先权日:2005-05-04
标 题:Thia-tetraazaacenaphthylene kinase inhibitors
发明人：BATTISTA KATHLEEN A; BIGNAN GILLES C; CONNOLLY PETER J; HAYDEN STUART; JOHNSON SIGMOND G; LIN RONGHUI; PANDEY NIRANJAN B; POWELL MARK T
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to novel thia-tetraazaacenaphthylene compounds of Formula (I): n nand pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of ATP-protein kinase interactions.