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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Hybrid anticancer agents: isothiocyanate-progesterone conjugates as chemotherapeutic agents and insights into their cytotoxicities.
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Hybrid anticancer agents: isothiocyanate-progesterone conjugates as chemotherapeutic agents and insights into their cytotoxicities.

机译：杂交抗癌剂：异硫氰酸酯 - 黄体酮缀合物作为化学治疗剂和洞察力的细胞毒性。

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摘要

New hybrid molecules of isothiocyanate and progesterone and their metal complexes were synthesized exhibiting promising anti-proliferative and pro-apoptotic activity against breast and prostate cancer cells. These metal complex compounds exploited an existing cellular transport pathway for delivery of cytotoxic isothiocyanate moiety across cell membrane resulting in the inhibition of cell viability and inducing apoptosis. The highest apoptotic action was shown by the copper complex, which was mediated through the inhibition of Akt signaling similar to the one shown by isothiocyanate compounds. Our results underscore the possible role of metal redox cycling, and thus it is likely will open newer avenues for further optimization for the synthesis of novel active compounds through appropriate isothiocyanate pharmacophores.
机译：合成了异硫氰酸异氰酸酯和孕酮及其金属配合物的新杂种分子，其具有对乳腺癌和前列腺癌细胞的有前途的抗增殖和促凋亡活性。 这些金属复合物化合物利用现有的细胞输送途径，用于跨细胞膜递送细胞毒性异硫氰酸酯部分，导致细胞活力抑制和诱导细胞凋亡。 铜络合物显示了最高的凋亡作用，其通过抑制与异硫氰酸酯化合物所示的Akt信号传导的抑制来介导。 我们的结果强调了金属氧化还原循环的可能作用，因此它可能会通过适当的异硫氰酸酯药物团来进一步优化新型活性化合物的进一步优化。

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