CAS: 477-30-5; (-)-Demecolcine

该化合物是一种化学化合物,被归类为一种以生物研究中使用和潜在治疗剂而闻名的可溶性衍生物,其特点是能够抑制微囊聚合物,这种聚合物会扰乱线性脊椎形成,使其在细胞分解和癌症研究中具有价值.Demecolcine通常被作为白色和脱白晶粉的白,并且可溶于二甲基硫氧化物(DMSO)和水中略微溶解的有机溶剂.该化合物具有反映其复杂结构的分子方程式,其中包括一个苯丙胺环和甲氧基组.由于其生物活动,已调查脱mecolcine在治疗某些类型的癌症和遗传障碍方面的潜在应用,尽管其使用往往受到毒性和副作用的限制.与许多化学物质一样,在实验室中与脱甲基二酚合作时,适当的处理和安全防范措施是必不可少的.

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CAS号14686-61-4 Formamide,N-met... | CAS号64-86-8 秋水仙碱 | CAS号477-27-0 原水仙碱 | CAS号3482-37-9 三甲基秋水仙酸 | CAS号3476-50-4 Trimethylcolchi... | CAS号74-88-4 碘甲烷 | CAS号186581-53-3 重氮甲烷 | CAS号518-11-6 COLCHICEINE, N-... | CAS号7359-91-3 (7S)-2-hydroxy-... | CAS号518-11-6 COLCHICEINE, N-... | CAS号14686-61-4 Formamide,N-met... | CAS号16892-03-8 Benzo[a]heptale... | CAS号7336-40-5 N-甲基-秋水仙碱 | CAS号7336-44-9 Demecolcine, N-... | CAS号76129-11-8 Benzo[a]heptale... | CAS号86436-33-1 N-Hydroxyacetyl...

合成工艺路线路线简述

    原秋水仙碱置于盐酸,乙醚,二氯甲烷,苯体系中,化学反应生成 脱羰秋水仙碱
    参考文献:Demecolcin和一些其他秋水仙碱衍生物的部分合成.秋番红花的物质及其衍生物.交流36
    标题:Demecolcin和一些其他秋水仙碱衍生物的部分合成.秋番红花的物质及其衍生物.交流36
    摘要:Demecolcin的配方已通过部分合成得到证明.脱乙酰基水杨碱可提供晶体.苯甲化合物.当用重氮甲烷甲基化时,得到n-苯甲酰-去乙酰-秋水仙碱和n-苯甲酰-异秋水仙碱的混合物,后者可以从中分离成晶体.用hcl裂解得到结晶.脱乙酰基-异秋水仙碱.克里斯特的母液.苯甲化合物反应生成粗制的脱乙酰基秋水仙碱和hcl,可从中通过酒石酸盐提纯纯碱.它尚未结晶.纯的去乙酰秋水仙碱部分甲基化,除其他外,产生了纯的德美霉素.描述了许多其他衍生物.
    DOI:10.1002/hlca.19540370104

    海关参考信息

    专利信息


    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-2025090698-A1
    优先权日:2018-11-27
    标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
    发明人:CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
    权利人:INDIAN INSTITUTE OF TECH INDORE
    摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:WO-2017100796-A1
    优先权日:2015-12-11
    标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
    权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
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    主要参考文献


    1: Gao Y, Ren J, Zhang L, Zhang Y, Wu X, Jiang H, Xu F, Yuan B, Yu X, Zhang J. The effects of demecolcine, alone or in combination with sucrose on bovine oocyte protrusion rate, MAPK1 protein level and c-mos gene expression level. Cell Physiol Biochem. 2014;34(6):1974-82. doi: 10.1159/000366393. Epub 2014 Nov 25. doi: 10.1111/rda.12246. Epub 2013 Oct 21. doi: 10.1089/cell.2011.0012. Epub 2011 Jul 8. doi: 10.1089/clo.2008.0044. Chinese. Epub 2008 Jan 30. Epub 2006 Apr 6. doi: 10.1089/clo.2007.0088. doi: 10.1017/S0967199414000537. Epub 2014 Oct 16. doi: 10.1111/j.1365-2184.2011.00734.x. doi: 10.1016/j.cellbi.2009.08.010. Epub 2009 Sep 2. doi: 10.1089/cell.2013.0051. Epub 2013 Nov 12.
    19: Ibáñez E, Albertini DF, Overström EW. Demecolcine-induced oocyte enucleation for somatic cell cloning: coordination between cell-cycle egress, kinetics of cortical cytoskeletal interactions, and second polar body extrusion. Biol Reprod. 2003 Apr;68(4):1249-58. Epub 2002 Oct 30.

    合成参考文献


    参考文献:10.1267/ahc.10037
    摘要:Chida K, Taguchi M. Localization of Alkaline Phosphatase and Cathepsin D during Cell Restoration after Colchicine Treatment in Primary Cultures of Fetal Rat Hepatocytes. Acta Histochem Cytochem. 2011 Jun 29;44(3):155–8.
    参考文献:10.1371/journal.pbio.1001099
    摘要:Wu G, Liu N, Rittelmeyer I, Sharma AD, Sgodda M, Zaehres H, Bleidißel M, Greber B, Gentile L, Han DW, Rudolph C, Steinemann D, Schambach A, Ott M, Schöler HR, Cantz T. Generation of Healthy Mice from Gene-Corrected Disease-Specific Induced Pluripotent Stem Cells. PLoS Biol. 2011 Jul 12;9(7):e1001099. doi: 10.1371/journal.pbio.1001099.
    参考文献:10.1155/2011/708450
    摘要:Kumar M, Kumar R, Tanwar M, Ghose S, Kaur J, Dada R. Cytogenetic and Clinical Assessment of a Family with Treacher Collins Syndrome. Case Reports in Medicine. 2011;2011():1–5. doi: 10.1155/2011/708450.
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