Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma.

摘要: Abstract No new and effective treatments have been approved for the treatment of esophageal squamous cell carcinoma (ESCC) in past decade. Cisplatin 5-fluoruracil are most commonly used drugs this disease. In order to develop a class our ESCC phenotypic screens, we began systematic approach generate novel compounds based on 2-oxo-1,2-dihydroquinoline-4-carboxamide fragment. Herein, report synthesis initial assessment 55 analogues two lines. Some active with IC50 values around 10 μM were tested three additional Our structure-activity relationships revealed remarkable alterations anti proliferative activities upon modest chemical modifications autophagy modulation is suggested mechanism action.