CAS: 25387-67-1; Sodium (S)-2-Hydroxy-2-(8-(Hydroxymethyl)-9-Oxo-9,11-Dihydroindolizino[1,2-B]Quinolin-7-yl)Butanoate

该化合物是来自Camptotheca cabuminata树树皮的天然藻类,其作用主要是作为抗癌剂的作用,它作为抗癌剂的作用,它作为异构物1抑制剂,它干扰DNA的复制和转录,最终导致癌症细胞迅速分解导致细胞死亡;钠盐形式在水溶液中强化其溶解性,使其更适合药物配方;盐展示一系列生物活动,包括对各种癌症细胞线的细胞毒性;其行动机制包括稳定Topope异构体1-DNA综合体,防止DNA线的重新定型,这对维护基因完整性至关重要;此外,还研究其结合疗法的潜力,以提高其他乳糖制剂的功效;然而,其临床用途往往受到诸如毒性和药物抗药性发展等问题的限制,因此有必要对其药性特性和配方战略进行持续研究.

结构式图片

欧盟法规

C&L通报

上下游产品

camptothecin

合成工艺路线路线简述

  • 合成目标产物 Sodium Camptothecin 主要起始原料 (+)-Camptothecin
  • (文献来源)合成步骤主要原料 (+)-Camptothecin
📜喜树碱 在 Sodium Hydroxide,水体系中,反应 2.0H,获得 20(S)-Camptothecin Sodium Salt
参考文献:Loading Of A Camptothecin Drug Into Colloidal Nanoparticles
标题:Loading Of A Camptothecin Drug Into Colloidal Nanoparticles
摘要:本发明涉及一种改进的制备含有羧酸形式的紫杉醇类药物的胶体纳米粒制剂的方法,以及一个试剂盒和一种药物组合物.

海关参考信息

专利信息


专利号:US-5633260-A
优先权日:1994-04-19
标 题 :11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof
发明人:HAUSHEER FREDERICK H; HARIDAS KOCHAT
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients. The present invention also claims 11,7-HECPT and 11,7-HMCPT compositions, the synthesis of 11,7-HECPT or 11,7-HMCPT, the methods of formulation of 11,7-HECPT or 11,7 -HMCPT, and the methods of use of 11,7-HECPT or 11,7-HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7-HECPT or 11,7-HMCPT formulations to humans with various forms of cancer. Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.

专利号:US-7687487-B2
优先权日:2007-04-19
标题 :Camptothecin-analog with a novel, “flippedâ€? lactone-stable, E-ring and methods for making and using same
发明人:HAUSHEER FREDERICK H
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:The present invention discloses: (i) a novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic aents, to subjects in need thereof.

专利号:EP-2007386-B1
优先权日:2006-04-19
标题 :Camptothecin-analog with a novel, flipped lactone-stable, e-ring and methods for making and using same
发明人:HAUSHEER FREDERICK H
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:The present invention discloses: (i) a novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flippedâ€? E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic aents, to subjects in need thereof.

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品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Ibrahim S, Gao D, Sinko PJ. Selective cytotoxicity and combined effects of camptothecin or paclitaxel with sodium-R-alpha lipoate on A549 human non-small cell lung cancer cells. Nutr Cancer. 2014;66(3):492-9. doi: 10.1080/01635581.2013.749290. Epub 2013 Sep 24.
2: Lauricella M, Calvaruso G, Giuliano M, Carabillò M, Emanuele S, Vento R, Tesoriere G. Synergistic cytotoxic interactions between sodium butyrate, MG132 and camptothecin in human retinoblastoma Y79 cells. Tumour Biol. 2000 Nov-Dec;21(6):337-48.

合成参考文献


摘要:Gan to Kagaku Ryoho. Cancer and Chemotherapy., 14(850), 1987 []
摘要:Progress in Medical Chemistry., 9(1), 1973
摘要:Cancer Chemotherapy Reports, Part 1., 56(515), 1972 []
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