苯并咪唑衍生物的抗肿瘤活性及构效关系研究

Antitumor Activity Evaluation and Structure-activity Relationship of Benzimidazole Derivatives

恶性肿瘤是严重威胁人类生命健康的疾病,随着其发病率和死亡率的不断上升,对抗肿瘤药物的开发提出了巨大的需求。作为核酸类似物的苯并咪唑衍生物,具有广谱的抗肿瘤活性,是抗肿瘤药物的优势骨架。近年来研究表明苯并咪唑衍生物对肝癌、肺癌、乳腺癌、肾癌、前列腺癌、宫颈癌等多种肿瘤细胞有良好的抗肿瘤效果。本文综述了苯并咪唑类衍生物与肿瘤靶点的构效关系,为设计新型分子靶向抗肿瘤药物提供了参考和依据。

The increasing morbidity and high mortality of cancer creates a great demand for the development of novel antineoplastics.Benzimidazole derivatives have broad spectrum of antitumor activities against liver cancer,lung cancer,breast cancer,kidney cancer,prostate cancer,cercival cancer and other tumors both in vitro and in vivo.Therefore,benzimidazole,a nucleotides analogy,has been known as the privileged scaffold and imperative pharmacophore for the development of novel antineoplastics.Thus,the present review mainly emphases on the structural requirement for antitumor potential of benzimidazole hybrids targeting several key antitumor targets.This information may provide an opportunity to design novel molecular targeted benzimidazole derivatives for the treatment of cancers.