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ANTICANCER ACTIVITIES OF A HETEROCYCLIC MOLECULE THAT SELECTIVELY STABILIZES G-QUADRUPLEX DNA
ANTICANCER ACTIVITIES OF A HETEROCYCLIC MOLECULE THAT SELECTIVELY STABILIZES G-QUADRUPLEX DNA
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机译:选择性稳定G-quaduplex DNA的杂环分子的抗癌活性
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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.
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