评价小分子嵌插剂的光谱、动力学和电泳模型(英文)

Models for Anti-tumor Evaluation and Intercalation Mechanism Investigation

发现新小分子DNA嵌插剂是改进肿瘤化疗的有效途径之一。抗肿瘤活性评价模型和嵌插机制研究模型是发现新小分子DNA嵌插剂的重要基础。本文描述了细胞和动物以外的模型,包括DOCK评分、紫外(UV)、荧光、圆二色散(CD)、相对粘度、熔点曲线、小分子与CT DNA堆叠动力学常数、小分子与CT DNA嵌插动力学常数、小分子嵌插剂和CT DNA复合物的稳定常数和凝胶色谱电泳模型。

For improving the cancer chemotherapy the discovery of new DNA intercalator is one of the effective approaches.The investigations have demonstrated the utility of the models in both evaluation of anti-tumor activity and identification of intercalation mechanism.This paper describes the DOCK score,ultraviolet（UV）,fluorescence,circular dichroism（CD）,relative viscosity,melting curve,kinetics in calf thymus（CT） DNA stacking of small molecule intercalator,kinetics in CT DNA intercalation of small molecule intercalator,interaction stabilizing the stacking complex of small molecule intercalator and CT DNA and the gel electrophoresis based models as well as their use in the identification of small molecule intercalating towards DNA.