6907-56-8Relevant articles and documents
Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents
Zhou, Yuanyuan,Yan, Wei,Cao, Dong,Shao, Mingfeng,Li, Dan,Wang, Fang,Yang, Zhuang,Chen, Yong,He, Linhong,Wang, Taijin,Shen, Mingsheng,Chen, Lijuan
, p. 1114 - 1125 (2017/08/02)
A series of novel 4-anilinoquinoline derivatives were synthesized and evaluated for their antiproliferative activities. Among them, 14h exhibited the most potent cytotoxic activity with IC50 values ranging from 1.5 to 3.9 nM against all tested cancer cell lines, and showed promising efficacy in multidrug resistant cancer cells. Flow cytometry assay, immune-fluorescence staining, microtubule dynamics assays and competition assays with EBI identified that 14h was a novel tubulin depolymerization agent by binding to the colchicine site. Importantly, in vivo efficacy evaluation of HCT116 xenograft model, 14h showed efficient antitumor activity without significant loss in body weight. All the results indicated that 14h could be a promising candidate for the treatment of cancer.
Design, synthesis, and biological evaluation of 2-arylethenylquinoline derivatives as multifunctional agents for the treatment of Alzheimer's disease
Wang, Xiao-Qin,Xia, Chun-Li,Chen, Shuo-Bin,Tan, Jia-Heng,Ou, Tian-Miao,Huang, Shi-Liang,Li, Ding,Gu, Lian-Quan,Huang, Zhi-Shu
, p. 349 - 361 (2015/05/06)
A series of new 2-arylethenylquinoline derivatives (4a1-4a12, 4b1-4b8, 4c1-4c4, 4d1-4d3 and 4e1-4e9) were designed, synthesized, and evaluated as potential multifunctional agents for the treatment of Alzheimer's disease (AD). In vitro studies showed that these synthetic compounds inhibited self-induced Aβ1-42 aggregation effectively ranged from 23.6% to 83.9% at the concentration of 20 μM, and acted as potential antioxidants and biometal chelators. Their structure-activity relationships were obtained and discussed. In particular, compound 4b1, the most active compound, displayed strong inhibitory activity with an IC50 value of 9.7 μM for self-induced Aβ1-42 aggregation, good antioxidative activity with a value of 3.9-fold of Trolox, potent inhibitory activity for cholinesterase with IC50 values of 0.2 μM and 64.1 μM against butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE), respectively. Besides, 4b1 was also capable of disassembling the self-induced Aβ1-42 aggregation fibrils with a ratio of 59.8% at 20 μM concentration, and had a good metal chelating activity. Taken together, these results suggest that compound 4b1 might be a promising lead compound for AD treatment.
