酚酰胺的半合成及其对 THP-1、Hela、HepG2 和 MCF-7 细胞系的细胞毒性。
Semi-synthesis of phenolic-amides and their cytotoxicity against THP-1, HeLa, HepG2 and MCF-7 cell lines.
机构信息
Center for Biomolecular Structure, Function and Application, Suranaree University of Technology, Nakhon Ratchasima, Thailand.
School of Chemistry, Institute of Science, Suranaree University of Technology, Nakhon Ratchasima, Thailand.
出版信息
Nat Prod Res. 2024 Jun;38(12):2069-2077. doi: 10.1080/14786419.2023.2241971. Epub 2023 Aug 1.
In the present study, we derivatized several hydroxycinnamic and hydroxybenzoic acids to phenolic amides (PAMs) one step BOP mediated amide coupling reactions. Fifteen PAMs were synthesized in >40% yields and were screened for their cytotoxic activities against four cancer cell lines: THP-1 (leukaemia), HeLa (cervical), HepG2 (liver), and MCF-7 (breast), in comparison to 5-flurouracil (5-FU). Four amides showed IC ranging from 5 to 55 µM against all four cell lines. In contrast, tetradecyl-gallic-amide () affected only THP-1 leukaemia cells with IC of 3.08 µM. The activities of these compounds support the promise of phenolic amides as anticancer agents.
在本研究中，我们将几种羟基肉桂酸和羟基苯甲酸衍生为酚酰胺（PAMs），通过 BOP 介导的酰胺偶联反应一步完成。合成了 15 种 PAMs，产率>40%，并对其进行了细胞毒性筛选，以评估其对四种癌细胞系（THP-1[白血病]、HeLa[宫颈]、HepG2[肝]和 MCF-7[乳腺]）的活性，与 5-氟尿嘧啶（5-FU）相比。四种酰胺对所有四种细胞系的 IC 范围为 5-55µM。相比之下，十四烷基没食子酰胺（）仅对 THP-1 白血病细胞有效，IC 为 3.08µM。这些化合物的活性支持酚酰胺作为抗癌剂的潜力。
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