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以杂合分子作为抗癌剂靶向DNA小沟

Targeting DNA Minor Groove by Hybrid Molecules as Anticancer Agents.

作者信息

Nekkanti Shalini, Tokala Ramya, Shankaraiah Nagula

机构信息

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037. India.

出版信息

Curr Med Chem. 2017;24(26):2887-2907. doi: 10.2174/0929867324666170523102730.

Abstract

Agents which can recognize and bind specific sequences of DNA offer selective therapy through the modulation of specific transcription factors or genes. Recently, there has been renewed interest in the field of anticancer minor groove binders. This may be attributed to the fact that many compounds of this class have demonstrated significant antitumor activity against a wide variety of cancers in recent clinical trials. This review will discuss the recent efforts to overcome the drawbacks of existing minor groove binding anticancer agents through rational drug design based on scaffolds with known antitumor activity.

摘要

能够识别并结合特定DNA序列的试剂可通过调节特定转录因子或基因来提供选择性治疗。最近,抗癌小沟结合剂领域重新引起了人们的关注。这可能归因于这一类的许多化合物在最近的临床试验中已证明对多种癌症具有显著的抗肿瘤活性。本综述将讨论最近基于具有已知抗肿瘤活性的支架通过合理药物设计来克服现有小沟结合抗癌剂缺点的研究工作。

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