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ANTICANCER ACTIVITIES OF A HETEROCYCLIC MOLECULE THAT SELECTIVELY STABILIZES G-QUADRUPLEX DNA

机译:选择性稳定G-quaduplex DNA的杂环分子的抗癌活性

摘要

Heterocyclic bis-triazolylcarbazole compound and/or derivatives thereof is provided which is water soluble and selectively induces and/ or stabilizes G-quadruplex DNA with or without the presence of monovalent cations/salts. Also provided is their process of preparation of said compounds and/or derivatives using a modular one-pot azide-alkyne cycloaddition. Said heterocyclic bis- triazolylcarbazole compound and/or derivatives thereof favour anyone or more stabilization of said G-quadruplexes (c-MYC, c-KIT1, c-KIT2, h-TELO) over duplex DNA with nM-µM binding affinity, cell cycle arrest at the G2/M phase and induction of apoptotic cell death of the cancer cells effectively by bis-triazolecarbazole derivative containing carboxamide side chains with terminal–NMe2 groups around the carbazole core. Heterocyclic bis-triazolylcarbazole compound and/or derivatives thereof of the present invention as small molecules targeting G-quadruplexes thus finds end use and application as potent anti-cancer drugs.
机译:提供了杂环双-三唑基咔唑化合物和/或其衍生物,其是水溶性的并且在存在或不存在一价阳离子/盐的情况下选择性地诱导和/或稳定G-四链体DNA。还提供了使用模块化一锅叠氮化物-炔烃环加成反应制备所述化合物和/或衍生物的方法。与具有nM-μM结合亲和力的双链DNA相比,所述杂环双-三唑基咔唑化合物和/或其衍生物有利于所述G-四链体(c-MYC,c-KIT1,c-KIT2,h-TELO)的任何或更多稳定作用。通过在羧甲基核心周围带有末端NMe2基团的含羧酰胺侧链的双三唑咔唑衍生物有效地阻滞在G2 / M期并诱导癌细胞凋亡。因此,本发明的杂环双-三唑基咔唑化合物和/或其衍生物作为靶向G-四链体的小分子,最终被用作有效的抗癌药物。

著录项

  • 公开/公告号IN2014KO01136A

    专利类型

  • 公开/公告日2016-08-26

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN1136/KOL/2014

  • 申请日2014-11-05

  • 分类号A61K31/40;

  • 国家 IN

  • 入库时间 2022-08-21 14:25:18

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