CAS: 20554-84-1; (3As,9Ar,10Ar,10Bs,E)-6,9A-Dimethyl-3-Methylene-3A,4,5,8,9,9A,10A,10B-Octahydrooxireno[2',3':9,10]Cyclodeca[1,2-B]Furan-2(3H)-One

上下游产品

木香烃内酯 Costunolide 553-21-9

(1S,2S,3S,10R,E)-3-(3-Hydroxyprop-1-En-2-yl)-6,10-Dimethyl-11-Oxabicyclo[8.1.0]Undec-6-En-2-Ol置于2,2,6,6-Tetramethyl-Piperidine-N-Oxyl,碘苯二乙酸体系中,用 二氯甲烷 用作溶剂,以85 %的收率获得小白菊内酯
参考文献:发现新型倍半萜内酯衍生物作为治疗溃疡性结肠炎的有效 Pkm2 激活剂
标题:发现新型倍半萜内酯衍生物作为治疗溃疡性结肠炎的有效 Pkm2 激活剂
摘要:丙酮酸激酶m2(pkm2)可显着影响th17和treg细胞的分化;因此,它被认为是 Uc 治疗的一个有前途的靶点.在此,设计,合成了五个系列的木香烯内酯(cos )衍生物,并进行了生物学评价.其中,D5对 T 细胞增殖表现出优异的免疫调节活性和有效的 Pkm2 激活活性.同时,已证实d5也能与pkm2的cys424共价相互作用.分子对接和分子动力学 (Md) 研究表明,D5的二氟环丙基衍生物通过与 Arg399 静电相互作用改善蛋白质-配体相互作用.此外,D5显着抑制 Th17 而非 Treg 细胞的分化,从而恢复 Th17/treg 平衡,这归因于抑制 Pkm2 介导的糖酵解.口服d5可改善小鼠模型中葡聚糖硫酸钠 (Dss) 和 2,4,6-三硝基苯磺酸 (Tnbs) 诱导的结肠炎症状.总的来说,D5有潜力被开发为新型抗 Uc 候选药物.
Doi:10.1021/acs.Jmedchem.2C01856

专利信息

专利号:US-2023270891-A1
优先权日:2020-09-16
标 题:Methods and Apparatuses for the Synthesis of Drug-Loaded Magnetic Micelle Aggregates
发明人：SOKOLOV KONSTANTIN; ZHANG MARIE; KIM CHANG SOO; NEVOZHAY DMITRY; ABURTO REBECA; PEHERE ASHOK; Pang lang; HAZLE JOHN; BAST ROBERT CLINTON
权利人:IMAGION BIOSYSTEMS INC
摘要:Liposomes have been used in technologies in biological, pharmaceutical, medical and nutritional applications because they can offer biocompatibility, biodegradability, reduced toxicity, and capacity for size and surface modifications. Traditionally, liposomes are prepared by multiple steps. However, multiple steps of preparation may cause a number of problems including low yield, high polydispersity, and poor morphology. Here, we synthesized liposomes containing magnetic iron oxide nanoparticle using one-pot, single step synthesis under ultra-sonication. We optimized the lipid compositions, sonication power, concentration of iron oxide nanoparticles, and antibody conjugation using Cu-free click chemistry. Furthermore, we incorporated doxorubicin inside magnetic liposomes for combined antibody targeting and magnetic guidance. Fluorescence imaging and quantification confirmed that antibody conjugated magnetic liposome showed high cell specific targeting that was enhanced by magnetic delivery.

专利号:US-10428082-B2
优先权日:2016-01-29
标题:Triazole derivatives of melampomagnolide B and methods of use thereof
发明人：JANGANATI VENUMADHAV; CROOKS PETER; PONDER JESSICA; JORDAN CRAIG
权利人:BIOVENTURES LLC; UNIV COLORADO REGENTS; THE REGENTS OF THE UNIV OF COLORADO A BODY
摘要:The present disclosure relates to triazole derivatives of melampomagnolide B, their synthesis, and their use as anti-cancer compounds.

专利号:US-2022162188-A1
优先权日:2019-01-15
标 题:Isoprenoids and methods of making thereof
发明人：WILLIAMS GAVIN; LUND SEAN; HALL RACHAEL
权利人:UNIV NORTH CAROLINA STATE
摘要:Disclosed are methods for preparing isoprenoid subunits, as well as methods of employing these isoprenoid subunits for the synthesis of isoprenoids. Also provided are isoprenoids prepared using the methods described herein.

专利号:US-2008031986-A1
优先权日:2005-12-09
标题:Protein kinase modulation by hops and acacia products
发明人：TRIPP MATTHEW L; BABISH JOHN G; BLAND JEFFREY S; HALL AMY J; KONDA VEERA; PACIORETTY LINDA M; DESAI ANU
权利人:METAPROTEOMICS LLC
摘要:Botanical compounds to modulate kinase activity are disclosed. The compounds and methods disclosed also inhibit expression of COX-2, inhibit synthesis of prostaglandins selectively in target cells, and inhibit inflammatory response selectively. The compositions contain at least one fraction isolated or derived from hops or Acacia.

专利号:US-8263139-B2
优先权日:2005-08-09
标 题 :Protein kinase modulation by hops and Acacia products
发明人：TRIPP MATTHEW L; BABISH JOHN G; PACIORETTY LINDA M; BLAND JEFFREY S; HALL AMY J; KONDA VEERA; DESAI ANU
权利人:TRIPP MATTHEW L; BABISH JOHN G; PACIORETTY LINDA M; BLAND JEFFREY S; HALL AMY J; KONDA VEERA; DESAI ANU; METAPROTEOMICS LLC
摘要:Botanical compounds to modulate kinase activity are disclosed. The compounds and methods disclosed also inhibit expression of COX-2, inhibit synthesis of prostaglandins selectively in target cells, and inhibit inflammatory response selectively. The compositions contain at least one fraction isolated or derived from hops or Acacia.

专利号:EP-4213810-A1
优先权日:2020-09-16
标题 :Methods and apparatuses for the synthesis of drug-loaded magnetic micelle aggregates