1543-31-3Relevant academic research and scientific papers
Synthesis, molecular modeling and anti-inflammatory screening of novel fluorinated quinoline incorporated benzimidazole derivatives using the Pfitzinger reaction
El-Feky, Said A.,Thabet, Hamdy Kh.,Ubeid, Mustafa T.
, p. 87 - 94 (2014/05/06)
Several new fluorinated quinoline derivatives were synthesized and tested for their anti-inflammatory and ulcerogenic effect. A docking study on the COX-2 binding pocket was carried out for the target compounds to rationalize the possible selectivity of them against COX-2 enzyme. The most active compounds (3, 2, 7 and 11) were found to be superior to celecoxib as they were devoid of any ulcerogenic activity. Compound 3a demonstrated the highest anti-inflammatory activity as well as the best binding profiles into the COX-2 binding site. Moreover, compounds 3-12 were screened for antibacterial activity and none of them showed noteworthy activity.
Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety
Li, Sai,Huang, Qiang,Liu, Yajing,Zhang, Xiaolong,Liu, Shuang,He, Chao,Gong, Ping
, p. 62 - 73 (2013/07/27)
A series of novel bisquinoline derivatives connected by a 4-oxy-3-fluoroaniline moiety were synthesized and evaluated for their in vitro antitumour activities against a panel of five cancer cell lines (H460, HT-29, MKN-45, U87MG, and SMMC-7721). Most of compounds tested showed a potent activity and high selectivity towards the H460 and MKN-45 cell lines. Among the compounds tested, six (15d, 15e, 15m, 15n, 16a, and 16i) were further examined for their c-Met kinase activity; the compounds showed high efficacy with IC 50 values in the single-digit nM range. An analysis of structure-activity relationships indicated that an unsubstituted or a halogen-substituted phenyl ring on the 2-arylquinoline-4-carboxamide moiety was favourable for antitumour activity.
Synthesis, characterization and antimicrobial studies of some new quinoline incorporated benzimidazole derivatives
Garudachari,Satyanarayana,Thippeswamy,Shivakumar,Shivananda,Hegde, Gurumurthy,Isloor, Arun M.
experimental part, p. 900 - 906 (2012/09/10)
Two new series of quinoline incorporated benzimidazole derivatives (4a-i and 8a-f) were synthesized from substituted aniline and isatin through multi-step reaction. 6-substituted-4-carboxyquinolines (3a,b and 7) were synthesized by multi component one pot
