当前位置: X-MOL 学术Chem. Data Collect. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of bioactive quinoline acting as anticancer agents and their mode of action using in silico analysis towards Aurora kinase A inhibitors
Chemical Data Collections Pub Date : 2021-08-25 , DOI: 10.1016/j.cdc.2021.100768
Kereyagalahally H Narasimhamurthy , Dileep Kumar M. Guruswamy , Chandra , Nichhapurada Kallesha , Basappa , Kanchugarakoppal S Rangappa

In the present investigation, novel quinolines have been synthesized and analyzed for their invitro cytotoxic activity against human colon cancer and lung cancer cells. Among the newly synthesized quinoline derivatives, 2-(3-chlorophenyl)-6,7-dimethoxyquinoline (Q6) showed considerable cytotoxic activity against human colon cancer (HCT116) and lung cancer (A549) cell lines with IC50 values of 25.5 ± 2.7 and 32 ± 4.7 μM respectively. Since these quinolines interacted with an Aurora kinase A, we carried out the molecular docking investigation and observed that this quinoline displayed inhibitory potentials. Overall, the compound Q6 was well suited to develop a newer quinolines-based anticancer medication, especially to block cell cycle arrest through Aurora kinase A inhibitors in human cancer.



中文翻译:

用作抗癌剂的生物活性喹啉的合成及其对极光激酶 A 抑制剂的计算机分析

在本研究中,合成了新型喹啉并分析了它们对人结肠癌和肺癌细胞的体外细胞毒活性。在新合成的喹啉衍生物中,2-(3-氯苯基)-6,7-二甲氧基喹啉 ( Q6 ) 对人结肠癌 (HCT116) 和肺癌 (A549) 细胞系显示出相当大的细胞毒活性,IC 50值为 25.5 ± 2.7和 32 ± 4.7 μM 分别。由于这些喹啉与极光激酶 A 相互作用,我们进行了分子对接研究并观察到这种喹啉显示出抑制潜力。总体而言,化合物Q6 非常适合开发一种新的基于喹啉的抗癌药物,特别是通过极光激酶 A 抑制剂在人类癌症中阻断细胞周期停滞。

更新日期:2021-08-29
down
wechat
bug