苯磺酰胺衍生物作为有效的微管蛋白靶向剂的合成及抗癌评估
Synthesis, anti-cancer evaluation of benzenesulfonamide derivatives as potent tubulin-targeting agents.
作者信息
Yang Jun, Yang Simin, Zhou Shanshan, Lu Dongbo, Ji Liyan, Li Zhongjun, Yu Siwang, Meng Xiangbao
机构信息
The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
出版信息
Eur J Med Chem. 2016 Oct 21;122:488-496. doi: 10.1016/j.ejmech.2016.07.002. Epub 2016 Jul 5.
A series of benzenesulfonamide derivatives were synthesized and evaluated for their anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferative and tubulin polymerization. Compound BA-3b proved to be the most potent compound with IC50 value ranging from 0.007 to 0.036 μM against seven cancer cell lines, and three drug-resistant cancer cell lines, which indicated a promising anti-cancer agent. The target tubulin was also verified by dynamic tubulin polymerization assay and tubulin intensity assay.
合成了一系列苯磺酰胺衍生物，并对其抗增殖活性以及与微管蛋白的相互作用进行了评估。这些新衍生物对细胞增殖和微管蛋白聚合表现出显著活性。化合物BA - 3b被证明是最有效的化合物，对七种癌细胞系和三种耐药癌细胞系的IC50值在0.007至0.036μM之间，这表明它是一种有前景的抗癌剂。还通过动态微管蛋白聚合试验和微管蛋白强度试验对目标微管蛋白进行了验证。
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