CAS: 71486-22-1; Vinorelbine

上下游产品

CAS号38390-45-3 脱水长春碱 | CAS号162652-95-1 长春氟宁

脱水长春碱置于n-溴代丁二酰亚胺(Nbs),三氟乙酸,Silver Tetrafluoroborate体系中,用 二氯甲烷,四氢呋喃 作为反应溶剂,化学反应 22.0H,以53%的收率获得产物长春瑞宾
参考文献:微管蛋白聚合的抑制剂:长春花碱,脱水长春碱和长春瑞滨与硫代秋水仙碱,鬼臼毒素和浆果赤霉素iii的杂合物的合成和生物学评估.
标题:微管蛋白聚合的抑制剂:长春花碱,脱水长春碱和长春瑞滨与硫代秋水仙碱,鬼臼毒素和浆果赤霉素iii的杂合物的合成和生物学评估.
摘要:描述了通过将脱水长春碱,长春瑞滨和长春碱与硫代秋水仙碱,鬼臼毒素和浆果赤霉素iii连接而获得的一系列新型杂合化合物.介绍了两种类型的二酰基间隔基.报道了杂合化合物对微管蛋白聚合的影响.结果突出了间隔物的长度的重要性.具有最佳体外活性的化合物的免疫荧光显微镜和流式细胞术测量可能会破坏细胞中的微管网络并阻止适当的纺锤体设备的形成,从而导致细胞周期停滞在g2 / M期.在人肺癌细胞系a549中测试了新合成的化合物.
DOI:10.1016/j.Bmc.2008.04.025

专利信息

专利号:US-5220016-A
优先权日:1991-07-29
标 题:Synthesis of navelbine analogs
发明人：MAGNUS PHILIP D; THURSTON LEE S
权利人:UNIV TEXAS
摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-7816544-B2
优先权日:2004-03-23
标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species
发明人：JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A
权利人:UNIV BOSTON
摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

专利号:WO-2024104433-A9
优先权日:2022-11-16
标 题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament
发明人：ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING
权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING
摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.