CAS: 1053655-94-9; Isoquinolin-6-Ylmethanamine

相似化合物

1396762-19-8 1158754-94-9 1053655-96-1

上下游产品

6-bromo-isoquinoline isoquinoline-6-carbonitrile

📜6-溴异喹啉置于盐酸,四(三苯基膦)钯,Palladium On Activated Charcoal,氢气体系中,用 乙醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 48.0H,反应生成(异喹啉-6-基)甲胺
参考文献:Design,Synthesis,And Evaluation Of Novel Porcupine Inhibitors Featuring A Fused 3-Ring System Based On The 'reversed' Amide Scaffold
标题:Design,Synthesis,And Evaluation Of Novel Porcupine Inhibitors Featuring A Fused 3-Ring System Based On The 'reversed' Amide Scaffold
摘要:The Wnt Signaling Pathway Is An Essential Signal Transduction Pathway Which Leads To The Regulation Of Cellular Processes Such As Proliferation,Differentiation And Migration. Aberrant Wnt Signaling Is Known To Have An Association With Multiple Cancers. Porcupine Is An Enzyme That Catalyses The Addition Of Palmitoleate To A Serine Residue In Wnt Proteins,A Process Which Is Required For The Secretion Of Wnt Proteins. Here We Report The Synthesis And Structure-Activity-Relationship Of The Novel Porcupine Inhibitors Based On A 'Reversed' Amide Scaffold. The Leading Compound 53 Was As Potent As The Clinical Compound Lgk974 In A Cell Based Stf Reporter Gene Assay. Compound 53 Potently Inhibited The Secretion Of Wnt3A,Therefore Was Confirmed To Be A Porcupine Inhibitor. Furthermore,Compound 53 Showed Excellent Chemical And Plasma Stabilities. However,The Clearance Of Compound 53 In Liver Microsomal Tests Was Moderate To High,And The Solubility Of Compound 53 Was Suboptimal. Collective Efforts Toward Further Optimization Of This Novel Tricyclic Template To Develop Better Porcupine Inhibitors Will Be Subsequently Undertaken And Reported In Due Course. (C) 2016 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2016.09.041

专利信息

专利号:US-2025129021-A1
优先权日:2023-09-19
标 题:Small molecule protein synthesis modulators
发明人：GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.