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首页> 外文期刊>RSC Advances >Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents
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Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents

机译：氟取代螺毒物唑啉的合成与生物学评价为潜在的抗病毒和抗癌剂

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Electrophilic fluorine-mediated dearomative spirocyclization has been developed to synthesize a range of fluoro-substituted spiro-isoxazoline ethers and lactones. The in vitro biological assays of synthesized compounds were probed for anti-viral activity against human cytomegalovirus (HCMV) and cytotoxicity against glioblastomas (GBM6) and triple negative breast cancer (MDA MB 231). Interestingly, compounds 4d and 4n showed significant activity against HCMV (IC _(50) ～ 10 μM), while 4l and 5f revealed the highest cytotoxicity with IC _(50) = 36 to 80 μM. The synthetic efficacy and biological relevance offer an opportunity to further drug-discovery development of fluoro-spiro-isoxazolines as novel anti-viral and anti-cancer agents.
机译：已经开发了亲电氟介导的DeapOmative Spircyclization以合成一系列氟取代的螺氧唑啉醚和内酯。探讨了合成化合物的体外生物测定，用于对人巨细胞病毒（HCMV）的抗病毒活性和针对胶质母细胞瘤（GBM6）和三重阴性乳腺癌（MDA MB 231）的细胞毒性。有趣的是，化合物4D和4N对HCMV（IC _（50）〜10μm）显示出显着的活性，而4L和5F揭示了IC _（50）= 36至80μm的最高细胞毒性。合成疗效和生物学相关性为进一步吸毒的氟螺毒素和抗病毒和抗癌剂的进一步吸毒发育的机会提供了进一步的药物发现。

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