CAS: 22042-71-3; 2-(4-Formylphenoxy)Acetic Acid

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CAS号123-08-0 4-羟基苯甲醛; 对羟基苯甲醛 | CAS号79-11-8 氯乙酸 | CAS号73620-18-5 (4-甲酰基苯氧基)乙酸甲酯 | CAS号276884-77-6 2-(4-甲酰基苯氧基)乙酸叔丁酯 | CAS号64-69-7 碘乙酸 | CAS号79-08-3 溴乙酸 | CAS号56-23-5 四氯化碳 | CAS号19360-67-9 4-(甲酸基甲氧基)苯甲酸 | CAS号29936-86-5 2-[4-(氨基羰基)苯氧基]乙酸 | CAS号50-00-0 甲醛 | CAS号201230-82-2 carbon monoxide | CAS号123-08-0 4-羟基苯甲醛; 对羟基苯甲醛 | CAS号73620-18-5 (4-甲酰基苯氧基)乙酸甲酯 | CAS号127812-08-2 5,10,15,20-四(4-... | CAS号17172-57-5 2-(4-formylphen... | CAS号88951-64-8 N-(4-bromopheny... | CAS号91345-17-4 3-[4-(carboxyme...

📜4-(乙氧基羰基甲氧基)苯甲醛置于sodium Hydroxide体系中,用 甲醇,水 用作溶剂,化学反应生成4-甲酰苯氧基乙酸
参考文献:芬那酯和布洛芬作为合成创新型靶向 Cox-2 抗炎药物的基本成分,经过彻底的生物药理学评估和计算机模拟研究
标题:芬那酯和布洛芬作为合成创新型靶向 Cox-2 抗炎药物的基本成分,经过彻底的生物药理学评估和计算机模拟研究
摘要:Cyclooxygenase-2 通过催化花生四烯酸转化为前列腺素,在炎症中发挥着至关重要的作用,使其成为主要的治疗目标.选择性 Cox-2 抑制剂代表了抗炎治疗的重大进展,可提高疗效并减少副作用.这项研究描述了从芬那酯和布洛芬等已上市药物中合成新型抗炎化合物.通过严格的测试,化合物和-表现出显着的选择性抑制作用,Ic 值为 0.07 至 0.09 μm,表明具有有效的药理活性.评估,特别是针对化合物的评估,显示出显着的抗炎作用.值得注意的是,与角叉菜胶组相比,它在 5 小时标记时表现出最高的爪子厚度抑制作用(58.62%),表明其减轻炎症的效力.此外,它表现出快速起效,在 1 小时标记处观测到 54.88% 的抑制.随后的镇痛功效,组织学特征和毒理学特性的综合评价表明,该化合物不会诱发胃溃疡,这与甲芬那酸相关的溃疡倾向相反.此外,通过分子建模,场排列和密度泛函理论等方法对化合物进行了
Doi:10.1016/j.Bioorg.2024.107393

专利信息

专利号:US-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人：HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

专利号:US-5877296-A
优先权日:1994-06-03
标题:Process for preparing conjugates of methyltrithio antitumor agents
发明人：HAMANN PHILIP ROSS; HINMAN LOIS; HOLLANDER IRWIN
权利人:AMERICAN CYANAMID CO
摘要:This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.

专利号:US-2004028702-A1
优先权日:2002-07-26
标 题:Muramic acid derivative compounds
发明人：MALETIC MILANA M; LEEMAN AARON H; SANTORELLI GINA M; WADDELL SHERMAN T
摘要:The present invention pertains to the combinatorial synthesis of antibacterial agents that inhibit the Mur-pathway enzymes involved in bacterial cell wall assembly. The method uses p-alkoxybenzylidene as the linker for the attachment of a derivatized muramic acid to the polymeric resin support. This intermediate becomes the starting point for the combinatorial synthesis, which in conjunction with split-pooling techniques allows rapid synthesis of diverse analogues for high-throughput screening (HTS). The invention is further directed to the libraries of these finished compounds that vary at the peptide, N-acyl and anomeric UDP positions.

专利号:US-2007128658-A1
优先权日:2005-11-14
标 题:Fluorescent dyes, methods and uses thereof
发明人：BLACKWELL HELEN E; BOWMAN MATTHEW D
权利人:BLACKWELL HELEN E; BOWMAN MATTHEW D
摘要:The present invention provides a method for identifying and characterizing candidate fluorescent molecules. This method involves the generation of spatially addressed arrays of heterocyclic compounds which are candidate fluorescent molecules. The spatially addressed array can be used to identify fluorescent molecules among the candidate molecules. The spatially addressed array can be used to determine the optical characteristics of one more candidate molecules. The invention also provides methods for making such arrays of heterocyclic compounds. In a specific embodiment, synthetic methods are provided for synthesis of triarylpyridines, particularly unsymmetric triarylpyridines. n preferred embodiments, the present invention provides novel heterocyclic fluorescent compounds having deazalumazine, cyanopyridine or pyrimidine cores. Heterocyclic fluorescent compounds of this invention are useful as dyes to label molecules such as nucleic acids, peptides and proteins, and particularly antibodies. In other embodiments, the novel heterocyclic fluorescent compounds are useful as dyes to label cellular compartments and organelles. The novel heterocyclic fluorescent compounds can also be used as sensors or indicators of specific metal ions, chemical warfare agents and pH.

专利号:US-5739116-A
优先权日:1994-06-03
标题:Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents

专利号:US-4696932-A
优先权日:1984-10-26
标题 :Biologically-active xanthine derivatives
发明人：JACOBSON KENNETH A; DALY JOHN W; KIRK KENNETH L
权利人:US HEALTH
摘要:Certain functionalized cogeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A 1 - and A 2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity. Some of these analogs, containing a distal amino- or carboxylic-functionalized chain, are suitable for synthesis of amino acid conjugates. The compounds of this invention are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.