Design, Synthesis and Anticancer Activity Studies of Novel Quinoline-Indole Derivatives

Abstract

( a 郑州大学基础医学院 郑州 450001) ( b 郑州大学化工学院 郑州 450001) ( c 郑州大学药学院 郑州 450001) 摘要 作为开发新型有效抗癌药物的进一步工作, 采用分子杂交策略和路易斯酸催化偶联反应设计合成了一系列新型 喹啉-吲哚类化合物. 使用噻唑蓝(MTT)法评估了所合成的化合物对人胃癌细胞(MGC-803)、人食管癌细胞(Kyse450)和 人结肠癌细胞(HCT-116)的体外抑制活性. 其中, 2-氯-4-(5-甲氧基-1H-吲哚-3-基)喹啉(9b)展示较好的体外抗肿瘤活性,

Direct Regioselective Hydro(hetero)arylation/Cyclocondensation Reactions of β-(2-Aminophenyl)-α,β-ynones by Means of Transition-Metal Catalysis/Brønsted Acid Synergism: Experimental Results and Computational Insights

“…There is a growing research activity toward a viable approach to the synthesis of quinolines bearing an indolyl substituent because of their significant pharmacological activities . A series of novel quinoline–indole derivatives were designed and synthesized as effective anticancer agents . Transition-metal-catalyzed C–H functionalization of indoles represents an area of extensive research .…”

Design, Synthesis and Biological Evaluation of [1,2,4]Triazolo[1,5-a]pyrimidine Indole Derivatives against Gastric Cancer Cells MGC-803 via the Suppression of ERK Signaling Pathway

“…There are many drugs containing indoles that have been approved by the FDA for the treatment of different human diseases, such as the anticancer drugs Panobinostat (HDAC inhibitor) [ 25 ] and Osimertinib (3rd EGFR tyrosine kinase inhibitor) [ 26 ], and the anti-inflammatory drug Indomethacin [ 27 ]. Therefore, indoles are widely considered as one class of dominant skeletons for the development of novel drugs [ 18 , 22 , 28 , 29 , 30 ]. In addition, indole biaryl structures have been widely used in the discovery of antitumor drugs.…”

“…Indazole-benzimidazole derivative 6 [ 28 ], as a tubulin polymerization inhibitor, exhibited potent inhibitory activities against four cancer cell lines (MCF-7, A549, Hela and B16-F10 cells) and one paclitaxel-resistant cancer cell line (A2780/T cells) at low nanomolar levels. Quinoline-indole derivative 7 [ 29 ] exhibited potent inhibitory potency on MGC-803, HCT-116 and KYSE450 cells (IC 50 = 0.58, 0.68 and 0.59 μM, respectively), and induced cell apoptosis and G2/M phase arrest ( Figure 2 ).…”