2,2-Dimethyl-6-(2-Oxopropyl)-4H-1,3-Dioxin-4-One置于ammonium Hydroxide体系中,用 乙醇,甲苯 用作溶剂,化学反应生成2,4-二羟基-6-甲基吡啶 参考文献:Small Molecule Inhibitors Of Anthrax Edema Factor 标题:Small Molecule Inhibitors Of Anthrax Edema Factor 摘要:Anthrax Is A Highly Lethal Disease Caused By The Gram-(+) Bacteria Bacillus Anthracis. Edema Toxin (Et) Is A Major Contributor To The Pathogenesis Of Disease In Humans Exposed To B. Anthracis. Et Is A Bipartite Toxin Composed Of Two Proteins Secreted By The Vegetative Bacteria,Edema Factor (Ef) And Protective Antigen (Pa). Our Work Towards Identifying A Small Molecule Inhibitor Of Anthrax Edema Factor Is The Subject Of This Letter. First We Demonstrate That The Small Molecule Probe 50-Fluorosulfonylbenzoyl 50-Adenosine (Fsba) Reacts Irreversibly With Ef And Blocks Enzymatic Activity. We Then Show That The Adenosine Portion Of Fsba Can Be Replaced To Provide More Drug-Like Molecules Which Are Up To 1000-Fold More Potent Against Ef Relative To Fsba,Display Low Cross Reactivity When Tested Against A Panel Of Kinases,And Are Nanomolar Inhibitors Of Ef In A Cell-Based Assay Of Camp Production. (C) 2017 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2017.11.040
专利号:US-4094878-A 优先权日:1976-07-14 标题 :Chemical synthesis of flavipucine 发明人:WENDLER NORMAN L; GIROTRA NARINDAR N; ZELAWSKI ZBIGNIEW S 权利人:MERCK & CO INC 摘要:A method for the total chemical synthesis of flavipucine employs the condensation of 4-hydroxy-6-methyl-2-pyridone with isobutylglyoxal in alkali alkoxide. The resulting alkali salt is acylated in both the 1' and 4 positions. Treatment of the 1',4-diacyloxy derivative with excess alkaline peroxide yields flavipucine.
专利号:US-8344118-B2 优先权日:2007-10-31 标 题 :Preparation and isolation of 5′ capped MRNA 发明人:KORE ANILKUMAR; MUTHIAN SHANMUGASUNDARAM; CHARLES IRUDAYA 权利人:APPLIED BIOSYSTEMS LLC; KORE ANILKUMAR; MUTHIAN SHANMUGASUNDARAM; CHARLES IRUDAYA 摘要:The synthesis of capped/tagged RNA, methods of use and kits providing same are contemplated. Tagged RNA permits isolation of RNA transcripts in vitro. The ability to isolate and purify capped RNA results in improved transcription and translation and provides a tool for identifying RNA-protein interactions. Such capped RNA finds use in therapeutic applications, diagnosis and prognosis and in the treatment of cancers and HIV.
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.