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首页> 美国卫生研究院文献>Molecules >Bimetallic Iron–Palladium Catalyst System as a Lewis-Acid for the Synthesis of Novel Pharmacophores Based Indole Scaffold as Anticancer Agents
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Bimetallic Iron–Palladium Catalyst System as a Lewis-Acid for the Synthesis of Novel Pharmacophores Based Indole Scaffold as Anticancer Agents

机译：双金属铁钯催化剂体系作为一种用于合成新型药物基的吲哚支架作为抗癌剂的甲酸酸

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The Friedel–Crafts reaction between substituted indoles as nucleophiles with chalcones-based benzofuran and benzothiophene scaffolds was carried out by employing a highly efficient bimetallic iron–palladium catalyst system. This catalytic approach produced the desired bis-heteroaryl products with low catalyst loading, a simple procedure, and with acceptable yield. All synthesized indole scaffolds 3a–3s were initially evaluated for their cytotoxic effect against human fibroblast BJ cell lines and appeared to be non-cytotoxic. All non-cytotoxic compounds 3a–3s were then evaluated for their anticancer activities against cervical cancer HeLa, prostate cancer PC3, and breast cancer MCF-7 cell lines, in comparison to standard drug doxorubicin, with IC50 values 1.9 ± 0.4 µM, 0.9 ± 0.14 µM and 0.79 ± 0.05 µM, respectively, and appeared to be moderate to weak anticancer agents. Fluoro-substituted chalcone moiety-containing compounds, 3b appeared to be the most active member of the series against cervical HeLa (IC50 = 8.2 ± 0.2 µM) and breast MCF-7 cancer cell line (IC50 = 12.3 ± 0.04 µM), whereas 6-fluroindol-4-bromophenyl chalcone-containing compound 3e (IC50 = 7.8 ± 0.4 µM) appeared to be more active against PC3 prostate cancer cell line.
机译：通过采用高效的双金属铁 - 钯催化剂体系进行基于基氨基硫酸的苯并呋喃和苯并噻吩支架的替代吲哚之间的Friedel-Crafts反应。该催化方法生产具有低催化剂负载，简单的程序和可接受的产率的所需的双杂芳基产品。最初评价所有合成的吲哚支架3A-3S针对人成纤维细胞BJ细胞系进行细胞毒性作用，并且似乎是非细胞毒性的。然后评估所有非细胞毒性化合物3A-3S对宫颈癌Hela，前列腺癌PC3和乳腺癌MCF-7细胞的抗癌活动，与标准药物多柔比星相比，IC50值1.9±0.4μm，0.9±0.9±分别为0.14μm和0.79±0.05μm，似乎是中等的抗癌剂。含氟取代的含氯酮部分的化合物，3b似乎是颈部Hela（IC50 = 8.2±0.2μm）和乳腺MCF-7癌细胞系列（IC50 = 12.3±0.04μm）的最活跃成员（IC50 = 12.3±0.04μm），而6含氟吲哚-4-溴苯基胆酮化合物3e（IC50 = 7.8±0.4μm）似乎对PC3前列腺癌细胞系更加活跃。

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