New 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinazoline and 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinoline Derivatives: Synthesis and Biological Evaluation as Novel Anticancer Agents by Targeting G-Quadruplex
作者:Jean Guillon、Marc Le Borgne、Vittoria Milano、Aurore Guédin-Beaurepaire、Stéphane Moreau、Noël Pinaud、Luisa Ronga、Solène Savrimoutou、Sandra Albenque-Rubio、Mathieu Marchivie、Haouraa Kalout、Charley Walker、Louise Chevallier、Corinne Buré、Eric Largy、Valérie Gabelica、Jean-Louis Mergny、Virginie Baylot、Jacky Ferrer、Yamina Idrissi、Edith Chevret、David Cappellen、Vanessa Desplat、Zsuzsanna Schelz、István Zupkó
DOI:10.3390/ph17010030
日期:——
series of quinoline derivatives, 6-phenyl-bis(3-dimethylaminopropyl)aminomethylphenylquinoline 13a proved to be the most active. G-quadruplexes (G4) stacked non-canonical nucleic acid structures found in specific G-rich DNA, or RNA sequences in the human genome are considered as potential targets for the development of anticancer agents. Then, as small aza-organic heterocyclic derivatives are well known
新型 2,4-双[(取代-氨基甲基)苯基]苯基喹唑啉 12 和 2,4-双[(取代-氨基甲基)苯基]苯基喹啉 13 的合成本文分六个步骤报道,从各种卤代喹唑啉-2,4-(1H,3H)-二酮或取代苯胺开始。在体外测定产品对一组乳腺 (MCF-7 和 MDA-MB-231) 、人贴壁宫颈 (HeLa 和 SiHa) 和卵巢 (A2780) 细胞系的抗增殖活性。二取代的 6-和 7-苯基-双(3-二甲基氨基丙基)氨基甲基苯基-喹唑啉 12b、12f 和 12i 对六种人类癌细胞系显示出最有趣的抗增殖活性。在喹啉衍生物系列中,6-苯基-双(3-二甲基氨基丙基)氨基甲基苯基喹啉 13a 被证明是最活跃的。在人类基因组中特定的富含 G 的 DNA 或 RNA 序列中发现的 G-四链体 (G4) 堆叠的非经典核酸结构被认为是开发抗癌剂的潜在靶标。然后,由于众所周知小的氮杂杂环衍生物可以靶向和稳定 G4 结构,因此已通过