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12-N-苯磺酰基-11-苦参酸衍生物是一类全新结构骨架、对柯萨奇病毒B3(CVB3)显示较好活性的化合物,但其作用机制尚不清楚。本研究在前期构效关系基础上设计合成了两类分子探针:一类是用于BIAcore垂钓探寻靶蛋白的苦参胺类探针;另一类是用于生物素亲和层析寻找靶蛋白的生物素酸苦参酯类探针。通过对其抗CVB3活性评价,发现生物素分子探针10a具有较好抗CVB3活性,IC_(50)值为0.8μmol·L~(-1),SI值为58.3。此类活性分子探针的成功构建为此类化合物靶标蛋白寻找与探索提供了关键的化学工具。
12-N-phenylsulfonyl-11-matrine derivatives are a new class of structural skeletons that show good activity against coxsackievirus B3 (CVB3), but the mechanism of action is not clear. In this study, two types of molecular probes were designed and synthesized based on the structure-activity relationship of the early stage: the first one is the matrine probe which is used to probe the target protein by BIAcore fishing; the other one is used to search target by biotin affinity chromatography Protein biotin kushen ester probe. The anti-CVB3 activity of the biotin molecule probe 10a was evaluated by its activity against CVB3. The IC 50 value of the probe was 0.8 μmol·L -1, and the SI value was 58.3. The successful construction of such active molecular probes has provided a key chemical tool for the search and exploration of such target proteins.