CAS: 53902-12-8; 2-(3-(3,4-Dimethoxyphenyl)Acrylamido)Benzoic Acid

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CAS号14737-89-4 (E)-3-(3,4-二甲氧基... | CAS号134-20-3 邻氨基苯甲酸甲酯

邻氨基苯甲酸置于哌啶体系中,用 甲苯 作为反应溶剂,化学反应 4.0H,反应生成 曲尼司特
参考文献:Synthesis,Bioactivity Evaluation,And Molecular Docking Study Of Tranilast Analogs As Anticancer Agents
标题:Synthesis,Bioactivity Evaluation,And Molecular Docking Study Of Tranilast Analogs As Anticancer Agents
摘要:摘要 开发治疗潜力更大,毒性更小的新药,以克服化疗在癌症治疗中的局限性,已被视为当务之急. 化疗在癌症治疗中的局限性.最近的 最近的研究表明,氨曲司特单独使用或与其他化疗药物联合使用时具有非常好的抗癌活性. 与其他化疗药物联合使用时具有非常好的抗癌活性.本研究旨在合成氨曲司特类似物,评估其体外抗癌活性,并将其与其他化疗药物结合使用. 本研究旨在合成氨曲司特类似物,评估体外抗癌活性,并与 Tgfβ1 靶点对接,寻找更强的抗癌药物.氨曲司特 (5A)和类似物(5B-F)是由蒽二酸衍生物,梅尔德伦酸和苯甲醛根据克诺文纳格尔法合成的 根据 Knoevenagel-Doebner 反应合成了曲安奈德(5A)和类似物(5B-F).这些化合物的体外 并使用 Autodocktools-1.5.6 与 Tgfβ1 靶标对接. 成功合成并分析了曲尼司特(5A)和七种类似物(5B-H)的结构. 其中四种类似物(5B-D,5F)对 Hepg2 和 Mcf-7 细胞株都有较强的抑制作用. 浓度为 100 μg/ml 时,其增殖抑制率在 41% 至 95% 之间. 氨曲司特(16.95% 和 22.64%).化合物 5F 是最有效的类似物,其 Ic50 = 27.57 μg/ml(hepg2)和 16.67 μg/ml(mcf-7). 与 Tgfβ1 靶点的结合亲和力(对接得分 ˗7.35 Kcal/mol).七种氨曲司特类似物中的四种具有较强的细胞毒性活性. 对 Hepg2 和 Mcf-7 细胞株的细胞毒性活性均强于母体化合物氨曲司特. 化合物氨曲司特.值得注意的是,化合物 5F 对 Tgfβ细胞株显示出最强的活性和非常好的结合亲和力. 亲和力,这表明该化合物具有作为抗癌剂进行进一步研究的潜力.
DOI:10.2174/0115701786268073230926160649

专利信息

专利号:US-8420850-B2
优先权日:2010-05-14
标 题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers
发明人：DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE
权利人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE; IBERHOSPITEX SA
摘要:The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.

专利号:US-2003138490-A1
优先权日:2001-09-08
标 题 :Synthesis and uses of polymer gel nanoparticle networks
发明人：HU ZHIBING; LU XIHUA; GAO JUN; PONDER BILL C; JOHN JOHN ST; MORO DANIEL G
摘要:Disclosed is a new class of nanostructured polymeric materials comprising polymer gel nanoparticles that are covalently bonded through functional groups on the surfaces of neighboring particles. These nanoparticles may be prepared as suspensions in an aqueous or, non-aqueous environment. These gels have two unique and different structural networks; the primary network comprises crosslinked polymer chains in each individual particle, while the secondary network is a system of crosslinked nanoparticles. Particular polymer gel nanoparticle network compositions disclosed herein may function as carriers for controlled delivery of pharmaceuticals or other chemical agents, gel sensors and other commercial applications.

专利号:WO-2023096715-A9
优先权日:2021-10-22
标 题:Immunomodulatory glycosphingolipids and methods of use thereof
发明人：KASPER DENNIS; OH SUNGWHAN
权利人:HARVARD COLLEGE
摘要:Provided herein are a subset of alpha-galactosylceramide (alpha-GC) compounds having improved immunomodulatory activity, particularly with respect to NKT cell number and activity. Also provided herein are methods of use of such compounds, including in the modulation of NKT cells and/or activity in vivo. Further provided are combinatorial synthesis methods for generating alpha-GC compounds of specifically defined structure and thereby generating pure preparations thereof.

专利号:US-2022125838-A1
优先权日:2019-02-11
标题 :Immunomodulatory glycosphingolipids and methods of use thereof
发明人：OH SUNGWHAN; KASPER DENNIS L; SONG HEEBUM; PARK SEUNG BUM
权利人:HARVARD COLLEGE; SEOUL NAT UNIV R&DB FOUNDATION
摘要:Provided herein are a subset of alpha-galactosylceramide (alpha-GC) compounds having improved immunomodulatory activity, particularly with respect to NKT cell number and activity. Also provided herein are methods of use of such compounds, including in the modulation of NKT cells and/or activity in vivo. Further provided are combinatorial synthesis methods for generating alpha-GC compounds of specifically defined structure and thereby generating pure preparations thereof.

专利号:US-2012059117-A1
优先权日:2010-05-14
标 题 :Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers

专利号:WO-2011141341-A1
优先权日:2010-05-14
标题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers