343-69-1Relevant articles and documents
Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma
Shahin, Mai I.,Roy, Joyeeta,Hanafi, Maha,Wang, Dongyao,Luesakul, Urarika,Chai, Yifeng,Muangsin, Nongnuj,Lasheen, Deena S.,Abou El Ella, Dalal A.,Abouzid, Khaled A.,Neamati, Nouri
, p. 516 - 530 (2018/06/15)
No new and effective treatments have been approved for the treatment of esophageal squamous cell carcinoma (ESCC) in the past decade. Cisplatin and 5-fluoruracil are the most commonly used drugs for this disease. In order to develop a new class of drugs effective in our ESCC phenotypic screens, we began a systematic approach to generate novel compounds based on the 2-oxo-1,2-dihydroquinoline-4-carboxamide fragment. Herein, we report on the synthesis and initial assessment of 55 new analogues in two ESCC cell lines. Some of the active analogues with IC50 values around 10 μM were tested in three additional cell lines. Our structure-activity relationships revealed remarkable alterations in the anti proliferative activities upon modest chemical modifications and autophagy modulation is a suggested mechanism of action.
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors
Cao, Jingrong,Gao, Huai,Bemis, Guy,Salituro, Francesco,Ledeboer, Mark,Harrington, Edmund,Wilke, Susanne,Taslimi, Paul,Pazhanisamy,Xie, Xiaoling,Jacobs, Marc,Green, Jeremy
scheme or table, p. 2891 - 2895 (2010/01/16)
A series of N-benzylated isatin oximes were developed as inhibitors of the mitogen-activated kinase, JNK3. X-ray crystallographic structures aided in the design and synthesis of novel, selective compounds, that inhibit JNK3, but not p38 MAP kinase and provided key insights into understanding the behavior of gatekeeper residue methionine-146 in determining target selectivity for this series.
Enantioselective synthesis of BMS-204352 (MaxiPost) using N-fluoroammonium salts of cinchona alkaloids (F-CA-BF4).
Zoute, Ludivine,Audouard, Christophe,Plaquevent, Jean-Christophe,Cahard, Dominique
, p. 1833 - 1834 (2007/10/03)
The enantioselective synthesis of a potent Maxi-K potassium channel opener (BMS-204352) mediated by N-fluoroammonium salts of cinchona alkaloids is described. Two synthetic pathways were evaluated. An ee as high as 88% was achieved (>99% after a single re