61421-82-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities
Ren, Yichang,Ruan, Yong,Cheng, Binbin,Li, Ling,Liu, Jin,Fang, Yuyu,Chen, Jianjun
, (2021/08/30)
A series of acridine and quinoline derivatives were designed and synthesized based on our previous work as novel tubulin inhibitors targeting the colchicine binding site. Among them, compound 3b exhibited the highest antiproliferative activity with an IC50 of 261 nM against HepG-2 cells (the most sensitive cell line). In addition, compound 3b was able to suppress the formation of HepG-2 colonies. Mechanism studies revealed that compound 3b effectively inhibited tubulin polymerization in vitro and disrupted microtubule dynamics in HepG-2 cells. Furthermore, compound 3b inhibited the migration of cancer cells in a dose dependent manner. Moreover, compound 3b induced cell cycle arrest in G2/M phase and led to cell apoptosis. Finally, docking studies demonstrated that compound 3b fitted nicely in the colchicine binding site of tubulin and overlapped well with CA-4. Collectively, these results suggested that compound 3b represents a novel tubulin inhibitor deserving further investigation.
Synthesis and?SAR study of?acridine, 2-methylquinoline and?2-phenylquinazoline analogues as?anti-prion agents
Cope,Mutter,Heal,Pascoe,Brown,Pratt,Chen
, p. 1124 - 1143 (2007/10/03)
Transmissible spongiform encephalopathies (TSEs) are thought to arise from aggregation of a protease resistant protein denoted PrPSc, which is a misfolded isoform of the normal cellular prion protein PrPC. Using virtual high-throughp
SPECTRAL AND LUMINESCENT PROPERTIES OF 9-ARYLAMINOACRIDINES
Budyka, M. F.,Fatkulbayanov, R. M.
, p. 1075 - 1080 (2007/10/02)
A study has been made of the influence of electronic and steric factors of the aromatic substituent in 9-arylaminoacridines on the behavior of these compounds when subjected to light quanta or electron impact.It has been shown that the introduction of don
