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苯并咪唑衍生物的抗肿瘤活性及构效关系研究
引用本文:牟杰,陈宁海,裴冬生. 苯并咪唑衍生物的抗肿瘤活性及构效关系研究[J]. 中国医药工业杂志, 2021, 0(3): 283-298
作者姓名:牟杰  陈宁海  裴冬生
作者单位:江苏省新药研究与临床药学重点实验室;徐州医科大学药学院
基金项目:国家自然科学基金项目(81872080、81572349);江苏省自然科学基金项目(BK20181148);江苏省高等学校大学生创新创业训练计划项目(201910313073Y和201910313098H);江苏高校品牌专业建设专项立项课题(Xjyppzx201608);徐州市科技计划项目(KC20245);江苏高校哲学社会科学研究项目(2020SJA1080);徐州医科大学药学院临床药学国家一流专业建设专项研究课题(LCYX202025)给予支持。
摘    要:
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...

关 键 词:苯并咪唑  抗肿瘤活性  构效关系  靶点

Antitumor Activity Evaluation and Structure-activity Relationship of Benzimidazole Derivatives
MOU Jie,CHEN Ninghai,PEI Dongsheng. Antitumor Activity Evaluation and Structure-activity Relationship of Benzimidazole Derivatives[J]. Chinese Journal of Pharmaceuticals, 2021, 0(3): 283-298
Authors:MOU Jie  CHEN Ninghai  PEI Dongsheng
Affiliation:(Jiangsu Key Lab of New Drug Research and Clinical Pharmacy,Xuzhou 221000;School of Pharmacy,Xuzhou Medical University,Xuzhou 221000)
Abstract:
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.
Keywords:benzimidazole  antitumor activity  structure-activity relationship  target
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