CAS: 104195-61-1; 10-Nitro-Camptothecin

该化合物是主要研究其在癌症治疗中潜在用途的合成化合物,属于野生植物衍生物类别,其作用机制以甲型异构体酶I抑制剂为名,这种抑制干扰了DNA复制和转录,导致癌症细胞死亡;鲁比坦(Rubitecan)展示了一种独特的化学结构,有助于其药理特性,包括其溶解性和稳定性;该化合物在各种临床前科和临床研究中进行了评估,展示了针对一系列肿瘤类型的活动;其药理学学衍生物,包括吸收,分布,代谢和排泄物,对于了解其治疗潜力和优化剂量疗法至关重要;此外,像许多抗癌剂一样,鲁比坦(Rubitecan)可能具有相关的副作用,需要在治疗期间进行仔细监测. 正在进行的研究旨在进一步阐明其功效和安全特征,并探索可能增强抗癌效果的混合疗法.

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    CAS号56008-61-8 2-氨基-5-硝基苯甲醛 | CAS号102978-40-5 4-乙基-7,8-二氢-4-羟... | CAS号104195-62-2 1H-Pyrano3,4:6,...

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      专利信息


      专利号:US-5321140-A
      优先权日:1990-12-20
      标 题 :Pyridinecarboxaldehyde D-ring intermediates useful for the synthesis of camptothecin and camptothecin analogs
      发明人：COMINS DANIEL L; BAEVSKY MATTHEW F
      权利人:UNIV NORTH CAROLINA STATE
      摘要:Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R 1 may be H, loweralkyl, loweralkoxy, or halo; R 2 , R 3 , R 4 , and R 5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

      专利号:WO-9325556-A1
      优先权日:1992-06-18
      标 题:Methods and intermediates for the asymmetric synthesis of camptothecin and camptothecin analogs

      专利号:DE-69330496-T2
      优先权日:1992-06-18
      标题:METHOD AND INTERMEDIATE PRODUCTS FOR THE ASYMMETRICAL SYNTHESIS OF CAMPTOTHECIN AND CAMPTOTHECIN ANALOGS

      专利号:JP-3499554-B2
      优先权日:1992-06-18
      标题:Methods and intermediates for asymmetric synthesis of camptothecin and camptothecin analogs

      专利号:JP-H07507795-A
      优先权日:1992-06-18
      标 题 :Methods and intermediates for asymmetric synthesis of camptothecin and camptothecin analogs

      专利号:EP-0646117-B1
      优先权日:1992-06-18
      标题:Methods and intermediates for the asymmetric synthesis of camptothecin and camptothecin analogs

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      合成参考文献


      参考文献:10.3892/ijmm.21.4.477
      摘要:Cao Z, Mendoza J, DeJesus A, Vardeman D, Giovanella B. Synthesis and antitumor activity of aromatic camptothecin esters. Int J Mol Med. 2008 Apr 01;(). doi: 10.3892/ijmm.21.4.477.
      参考文献:10.1007/s11912-011-0176-x
      摘要:Stacchiotti S, Casali PG. Systemic therapy options for unresectable and metastatic chordomas. Curr Oncol Rep. 2011 Aug;13(4):323–30. doi: 10.1007/s11912-011-0176-x.
      参考文献:10.1007/s40487-016-0018-y
      摘要:Heery CR. Erratum to: Chordoma: The Quest for Better Treatment Options. Oncology and Therapy. 2016 Apr 20;4(1):53–5. doi: 10.1007/s40487-016-0018-y.
      参考文献:10.1023/b:drug.0000006176.84915.71
      摘要:Miller KD, Soule SE, Haney LG, Guiney P, Murry DJ, Lenaz L, Sun SL, Sledge GW. A phase II study of 9-nitro-camptothecin in patients with previously treated metastatic breast cancer. Invest New Drugs. 2004 Jan;22(1):69–73. doi: 10.1023/b:drug.0000006176.84915.71.
      参考文献:10.1016/s1091-255x(99)80084-5
      摘要:Litvak DA, Papaconstantinou HT, Evers BM, Townsend CM. Targeting molecular pathways with camptothecin as novel therapy for gastric cancer. Journal of Gastrointestinal Surgery. 1999 Nov;3(6):618–24. doi: 10.1016/s1091-255x(99)80084-5.
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