【摘要】 目的设计合成新型1,5-二取代吡唑-3-甲酰胺类化合物,并对其抗ALK5活性进行初步评价。方法以取代的苯乙酮及草酸二甲酯为原料,经多步反应合成目标化合物,用化学发光法检测报告基因表达产物萤火虫萤光素酶活性,计算化合物对ALK5的抑制率。结果与结论共合成15个未见文献报道的新化合物,其结构经IR1、H-NMR和MS确证。初步生物活性评价结果显示化合物4g具有一定的抗ALK5活性。更多还原

【Abstract】 Aim To design and synthesize novel 1,5-diarylpyrazole-3-carboxamide derivatives,and to assay their activities of inhibiting ALK5.Methods The target compounds were synthesized from substituted acetophenone and dimethyl oxalate and the activities of inhibiting ALK5 were assayed by luciferase reporter system transfected in 293 cells.Results and conclusion Fifteen new compounds were synthesized and their structures were confirmed by IR,()~1H-NMR and MS.The primary biological tests showed that compound 4g exhibited some ALK5 inhibitory activity.更多还原