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Carbocyanines for G-Quadruplex DNA Stabilization and Telomerase Inhibition

机译:碳菁用于G-四链体DNA稳定和端粒酶抑制

摘要

Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.
机译:本文描述了选择性结合G-四链体DNA复合物,特别是在癌细胞中表达的四链体的花菁,及其制备和使用方法。花青可以是对称或不对称的链花青,半花青,闭链花青或其组合。花青优选被一个或多个基团取代,所述基团最小化或防止花青的聚集和/或抑制花青与双链DNA的结合。可以将一种或多种花青与一种或多种药物赋形剂和/或载体一起配制以制备适合于施用于患者,特别是人类患者的药物组合物。本文所述的化合物和组合物可用于治疗以G-四链体DNA的表达为特征的疾病或病症,例如癌症。

著录项

  • 公开/公告号US2014142147A1

    专利类型

  • 公开/公告日2014-05-22

    原文格式PDF

  • 申请/专利权人 MAGED HENARY;W. DAVID WILSON;

    申请/专利号US201214233044

  • 发明设计人 MAGED HENARY;W. DAVID WILSON;

    申请日2012-07-18

  • 分类号C09B23/06;

  • 国家 US

  • 入库时间 2022-08-21 16:08:35

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