通过抑制微管蛋白聚合合成具有抗癌活性的 2-亚苄基茚满酮
Synthesis and anticancer activity of 2-benzylidene indanones through inhibiting tubulin polymerization.
机构信息
CSIR, Central Institute of Medicinal and Aromatic Plants, Kukrail Picnic Spot Road, Lucknow 226 015, UP, India.
出版信息
Bioorg Med Chem. 2012 May 1;20(9):3049-57. doi: 10.1016/j.bmc.2012.02.057. Epub 2012 Mar 14.
In an attempt to discover a potent and selective anticancer agent, gallic acid has been modified to benzylidene indanones as tubulin polymerization inhibitors. These compounds were evaluated against several human cancer cell lines and also evaluated for inhibition of tubulin polymerase in in vitro assays. Three of the analogues exhibited strong cytotoxicity against human cancer cell lines IC(50)=10-880 nM and also showed tubulin polymerization inhibition (IC(50)=0.62-2.04 μM). Compound 9j, the best candidate of the series was found to be non-toxic in acute oral toxicity in Swiss-albino mice up to 1000 mg/kg dose.
为了发现一种有效且选择性的抗癌药物，人们对没食子酸进行了修饰，将其制成苯丁烯基茚满酮类化合物，作为微管聚合抑制剂。这些化合物被评估了对几种人类癌细胞系的活性，同时也评估了它们在体外试验中对微管聚合酶的抑制作用。其中三个类似物对人类癌细胞系表现出很强的细胞毒性（IC50=10-880 nM），并且也显示出微管聚合抑制作用（IC50=0.62-2.04 μM）。在急性口服毒性试验中，在瑞士白化小鼠中，该系列中最好的候选化合物 9j 被发现最高剂量达 1000 mg/kg 时无毒性。
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