CAS: 763114-04-1; Tert-Butyl 4-(2-Fluoro-5-((4-Oxo-3,4-Dihydrophthalazin-1-yl)Methyl)Benzoyl)Piperazine-1-Carboxylate

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2-fluoro-5-[(4'-oxo-3'H-phthalazin-1'-yl)methyl]benzoic acid 1-t-Butoxycarbonylpiperazine o-carboxybenzaldehyde 2-fluoro-5-formylbenzonitrile4-[4''-fluoro-3''-(piperazine-1'''-carbonyl)benzyl]-2H-phthalazin-1-one 1-cyclopropyl-2-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)ethane-1,2-dione 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-2-phenylethane-1,2-dione 1-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-3,3-dimethylbutane-1,2-dione

2-Fluoro-5-[(3-Oxo-2-Benzofuran-1-Ylidene)Methyl]Benzoic Acid置于o-(1H-Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Hexafluorophosphate,一水合肼,三乙胺体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 145.0H,反应生成 4-[2-氟-5-[(4-氧代-3,4-二氢酞嗪-1-基)甲基]苯甲酰基]哌嗪-1-羧酸叔丁酯
参考文献:Synthesis And Evaluation Of A Radioiodinated Tracer With Specificity For Poly(Adp-Ribose) Polymerase-1 (Parp-1) In Vivo
标题:Synthesis And Evaluation Of A Radioiodinated Tracer With Specificity For Poly(Adp-Ribose) Polymerase-1 (Parp-1) In Vivo
摘要:Interest In Nuclear Imaging Of Poly(Adp-Ibose) Polymerase-1 (Parp-1) Has Grown In Recent Years Due To The Ability Of Parp-1 To Act As A Biomarker For Glioblastoma And Increased Clinical Use Of Parr-1 Inhibitors. This Study Reports The Identification Of A Lead Iodinated Analog 5 Of The Clinical Parp-1 Inhibitor Olaparib As A Potential Single-Photon Emission Computed Tomography (Spect) Imaging Agent. Compound 5 Was Shown To Be A Potent Parp-1 Inhibitor In Cell-Free And Cellular Assays,And It Exhibited Mouse Plasma Stability But Approximately 3-Fold Greater Intrinsic Clearance When Compared To Olaparib. An (123)-I-Labeled Version Of 5 Was Generated Using Solid State Halogen Exchange Methodology. Ex Vivo Biodistribution Studies Of [i-123]5 In Mice Bearing Subcutaneous Glioblastoma Xenografts Revealed That The Tracer Had The Ability To Be Retained In Tumor Tissue And Bind To Parp-1 With Specificity. These Findings Support Further Investigations Of [i-123]5 As A Noninvasive Parp-1 Spect Imaging Agent.
DOI:10.1021/acs.Jmedchem.5B01324