• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

吖啶化合物作为黑色素瘤联合靶向化学-放射性核素治疗潜在药物的设计、合成及初步生物学评价

Design, synthesis and preliminary biological evaluation of acridine compounds as potential agents for a combined targeted chemo-radionuclide therapy approach to melanoma.

作者信息

Desbois Nicolas, Gardette Maryline, Papon Janine, Labarre Pierre, Maisonial Aurélie, Auzeloux Philippe, Lartigue Claire, Bouchon Bernadette, Debiton Eric, Blache Yves, Chavignon Olivier, Teulade Jean-Claude, Maublant Jean, Madelmont Jean-Claude, Moins Nicole, Chezal Jean-Michel

机构信息

Univ Clermont 1, UFR Pharmacie, Clermont-Ferrand F-63001, France.

出版信息

Bioorg Med Chem. 2008 Aug 15;16(16):7671-90. doi: 10.1016/j.bmc.2008.07.015. Epub 2008 Jul 10.

DOI:10.1016/j.bmc.2008.07.015
PMID:18656367
Abstract

Various iodo-acridone and acridine carboxamides have been prepared and evaluated as agents for targeted radionuclide and/or chemotherapy for melanoma, due to their structural similarity to benzamides which are known to possess specific affinity for melanin. Three of these carboxamides selected for their in vitro cytotoxic properties were radioiodinated with [(125)I]NaI at high specific activity. Biodistribution studies carried out in B16F0 murine melanoma tumour-bearing mice highlighted that acridone 8f and acridine 9d, presented high, long-lasting tumour concentrations together with an in vivo kinetic profile favourable to application in targeted radionuclide therapy.

摘要

由于各种碘代吖啶酮和吖啶羧酰胺与已知对黑色素具有特异性亲和力的苯甲酰胺结构相似，因此已被制备并评估为用于黑色素瘤的靶向放射性核素和/或化疗的药物。选择其中三种具有体外细胞毒性的羧酰胺，用高比活度的[(125)I]NaI进行放射性碘化。在携带B16F0小鼠黑色素瘤肿瘤的小鼠中进行的生物分布研究表明，吖啶酮8f和吖啶9d在肿瘤中具有高且持久的浓度，并且其体内动力学特征有利于在靶向放射性核素治疗中应用。

相似文献

1
Design, synthesis and preliminary biological evaluation of acridine compounds as potential agents for a combined targeted chemo-radionuclide therapy approach to melanoma.吖啶化合物作为黑色素瘤联合靶向化学-放射性核素治疗潜在药物的设计、合成及初步生物学评价
Bioorg Med Chem. 2008 Aug 15;16(16):7671-90. doi: 10.1016/j.bmc.2008.07.015. Epub 2008 Jul 10.
2
Synthesis and preliminary evaluation of the new water-soluble radioactive platinum(IV) complexes.新型水溶性放射性铂（IV）配合物的合成与初步评价
J Inorg Biochem. 2004 Mar;98(3):553-9. doi: 10.1016/j.jinorgbio.2003.12.021.
3
Evaluation of new iodinated acridine derivatives for targeted radionuclide therapy of melanoma using 125I, an Auger electron emitter.评估新型碘代吖啶衍生物作为 125I（一种俄歇电子发射体）用于黑色素瘤靶向放射性核素治疗的效果。
Invest New Drugs. 2011 Dec;29(6):1253-63. doi: 10.1007/s10637-010-9471-x. Epub 2010 Jun 22.
4
Rational design, synthesis, and biological evaluation of bis(pyrimido[5,6,1-de]acridines) and bis(pyrazolo[3,4,5-kl]acridine-5-carboxamides) as new anticancer agents.新型抗癌剂双（嘧啶并[5,6,1 - de]吖啶）和双（吡唑并[3,4,5 - kl]吖啶 - 5 - 甲酰胺）的合理设计、合成及生物学评价
J Med Chem. 2004 Oct 7;47(21):5244-50. doi: 10.1021/jm049706k.
5
Synthesis, radiosynthesis, and biological evaluation of new proteasome inhibitors in a tumor targeting approach.以肿瘤靶向方法进行新型蛋白酶体抑制剂的合成、放射性合成及生物学评价。
J Med Chem. 2008 Feb 28;51(4):1043-7. doi: 10.1021/jm701419g. Epub 2008 Feb 1.
6
Melanoma affinity in mice and immunosuppressed sheep of [(125)I]N-(4-dipropylaminobutyl)-4-iodobenzamide, a new targeting agent.新型靶向剂[(125)I]N-(4-二丙基氨基丁基)-4-碘苯甲酰胺在小鼠和免疫抑制绵羊体内的黑色素瘤亲和力
Nucl Med Biol. 2008 Oct;35(7):783-91. doi: 10.1016/j.nucmedbio.2008.07.003.
7
Synthesis, in vitro binding and biodistribution in B16 melanoma-bearing mice of new iodine-125 spermidine benzamide derivatives.新型碘-125亚精胺苯甲酰胺衍生物的合成、体外结合及在荷B16黑色素瘤小鼠体内的生物分布
Nucl Med Biol. 2005 May;32(4):377-84. doi: 10.1016/j.nucmedbio.2005.02.004.
8
Design, synthesis, and biological properties of new bis(acridine-4-carboxamides) as anticancer agents.新型双（吖啶-4-甲酰胺）类抗癌剂的设计、合成及生物学特性
J Med Chem. 2003 Jul 3;46(14):3109-15. doi: 10.1021/jm030820x.
9
Evaluation of radiolabeled (hetero)aromatic analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for imaging and targeted radionuclide therapy of melanoma.用于黑色素瘤成像和靶向放射性核素治疗的 N-(2-二乙氨基乙基)-4-碘苯甲酰胺的放射性标记（杂）芳族类似物的评估
J Med Chem. 2008 Jun 12;51(11):3133-44. doi: 10.1021/jm701424g. Epub 2008 May 16.
10
Evaluation of apoptotic effect of cyclic imide derivatives on murine B16F10 melanoma cells.评价环状酰亚胺衍生物对鼠 B16F10 黑素瘤细胞的凋亡作用。
Bioorg Med Chem. 2011 Nov 1;19(21):6285-91. doi: 10.1016/j.bmc.2011.09.008. Epub 2011 Sep 10.

引用本文的文献

1
Auger electrons for cancer therapy - a review.用于癌症治疗的俄歇电子——综述
EJNMMI Radiopharm Chem. 2019 Oct 11;4(1):27. doi: 10.1186/s41181-019-0075-2.
2
Synthesis and Biological Evaluation of New Quinoxaline Derivatives of ICF01012 as Melanoma-Targeting Probes.ICF01012新型喹喔啉衍生物作为黑色素瘤靶向探针的合成及生物学评价
ACS Med Chem Lett. 2014 Feb 20;5(5):468-73. doi: 10.1021/ml400468x. eCollection 2014 May 8.
3
Evaluation of two (125)I-radiolabeled acridine derivatives for Auger-electron radionuclide therapy of melanoma.
两种（125）I 放射性标记吖啶衍生物用于黑色素瘤俄歇电子放射性核素治疗的评估
Invest New Drugs. 2014 Aug;32(4):587-97. doi: 10.1007/s10637-014-0086-5. Epub 2014 Apr 2.
4
Microwave-assisted improved synthesis of pyrrolo[2,3,4-kl]acridine and dihydropyrrolo[2,3,4-kl]acridine derivatives catalyzed by silica sulfuric acid.微波辅助硅胶硫酸催化合成吡咯并[2,3,4-kl]吖啶和二氢吡咯并[2,3,4-kl]吖啶衍生物。
Molecules. 2013 Jan 28;18(2):1613-25. doi: 10.3390/molecules18021613.
5
Evaluation of new iodinated acridine derivatives for targeted radionuclide therapy of melanoma using 125I, an Auger electron emitter.评估新型碘代吖啶衍生物作为 125I（一种俄歇电子发射体）用于黑色素瘤靶向放射性核素治疗的效果。
Invest New Drugs. 2011 Dec;29(6):1253-63. doi: 10.1007/s10637-010-9471-x. Epub 2010 Jun 22.
6
Preclinical evaluation of an 131I-labeled benzamide for targeted radiotherapy of metastatic melanoma.放射性碘标记苯甲酰胺用于转移性黑色素瘤靶向放射治疗的临床前评估。
Cancer Res. 2010 May 15;70(10):4045-53. doi: 10.1158/0008-5472.CAN-09-4414. Epub 2010 May 4.
7
Melanin-targeted preclinical PET imaging of melanoma metastasis.黑色素瘤转移的黑色素靶向临床前正电子发射断层显像（PET）成像
J Nucl Med. 2009 Oct;50(10):1692-9. doi: 10.2967/jnumed.109.066175. Epub 2009 Sep 16.