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新型三嗪类似物作为抗癌剂的合成、体外评价及其与牛血清白蛋白的相互作用研究

Synthesis and in vitro evaluation of novel triazine analogues as anticancer agents and their interaction studies with bovine serum albumin.

作者信息

Singla Prinka, Luxami Vijay, Paul Kamaldeep

机构信息

School of Chemistry and Biochemistry, Thapar University, Patiala 147 004, India.

School of Chemistry and Biochemistry, Thapar University, Patiala 147 004, India.

出版信息

Eur J Med Chem. 2016 Jul 19;117:59-69. doi: 10.1016/j.ejmech.2016.03.088. Epub 2016 Apr 3.

Abstract

A novel series of triazine-benzimidazole analogs has been designed and synthesized for their in vitro anticancer activities. Four compounds (6, 16, 17 and 20) were identified as highly potent anticancer agents against 60 human cancer cell lines with GI50 in the nanomolar range. To improve the drug applications toward cancer cells, there is a need to couple these compounds to some carrier macromolecules. Following this approach, the interaction between triazine-benzimidazole analogues and bovine serum albumin (BSA) has been investigated with UV-Visible and fluorescence spectroscopic methods under physiological conditions. The observed fluorescence quenching indicates that these compounds could efficiently bind with BSA and be transported to the target site.

摘要

设计并合成了一系列新型的三嗪 - 苯并咪唑类似物,以研究其体外抗癌活性。四种化合物(6、16、17和20)被鉴定为对60种人类癌细胞系具有高效抗癌活性,其半数生长抑制浓度(GI50)在纳摩尔范围内。为了改善这些化合物对癌细胞的药物应用,需要将它们与一些载体大分子偶联。按照这种方法,在生理条件下,采用紫外 - 可见光谱和荧光光谱法研究了三嗪 - 苯并咪唑类似物与牛血清白蛋白(BSA)之间的相互作用。观察到的荧光猝灭表明这些化合物能够有效地与BSA结合并转运到靶位点。

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