新型无碱性侧链 DNA 嵌入剂作为有效的抗肿瘤药物：苯并[c,d]吲哚-丙二腈衍生物的设计、合成与评价。
Novel DNA intercalators without basic side chains as efficient antitumor agents: design, synthesis and evaluation of benzo-[c,d]-indol-malononitrile derivatives.
机构信息
State Key Laboratory of Fine Chemicals, Dalian University of Technology, PO Box 89, 158 Zhongshan Road, Dalian 116012, China.
出版信息
Bioorg Med Chem. 2010 May 1;18(9):3279-84. doi: 10.1016/j.bmc.2010.03.017. Epub 2010 Mar 21.
Several 2-(substituted benzo[c,d]indol-2(1H)-ylidene)malononitriles have been designed and synthesized. Their DNA binding, antitumor and DNA damaging properties were evaluated. All the compounds exhibited efficient antitumor activities with preference to be against the tumor cell line 7721 rather than the tumor cell line MCF-7. Compound 1f could intercalate into DNA entirely presumably by the good conjugation of carbonyl group with benzo[c,d]indol moiety. What's more, 1f exhibited potent toxicity against MCF-7 cells with IC(50) at 0.003 microM and against 7721 cells at 0.115 microM, respectively.
设计并合成了几种 2-（取代苯并[c，d]吲哚-2（1H）亚基）丙二腈。评估了它们的 DNA 结合、抗肿瘤和 DNA 损伤特性。所有化合物均表现出高效的抗肿瘤活性，优先针对肿瘤细胞系 7721，而不是肿瘤细胞系 MCF-7。化合物 1f 可以通过羰基与苯并[c，d]吲哚部分的良好共轭完全嵌入 DNA。此外，1f 对 MCF-7 细胞的毒性较强，IC50 分别为 0.003 μM 和对 7721 细胞的 IC50 为 0.115 μM。
Zotero 插件