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多环芳烃类化合物用于抗癌药物开发的合成、亲电取代及构效关系研究

Synthesis, electrophilic substitution and structure-activity relationship studies of polycyclic aromatic compounds towards the development of anticancer agents.

作者信息

Banik B K, Becker F F

机构信息

Department of Molecular Pathology, The University of Texas, M.D. Anderson Cancer Center, Box-89, 1515 Holcombe Blvd., Houston, TX 77030, USA.

出版信息

Curr Med Chem. 2001 Oct;8(12):1513-33. doi: 10.2174/0929867013372120.

Abstract

Polycyclic aromatic hydrocarbons (PAH) are considered potentially carcinogenic. Substituted PAH derivatives, in contrast, may serve as anticancer agents, and as chemotherapeutics. This article presents a review of their use. Particular emphasis is placed on the synthesis of these new compounds, electrophilic substitution reactions and novel synthetic methodologies developed in our laboratory. Based on numerous reports and the data available, we believe that DNA-intercalating and membrane-interacting sites are the target for their effects.

摘要

多环芳烃(PAH)被认为具有潜在致癌性。相比之下,取代的PAH衍生物可作为抗癌剂和化学治疗剂。本文对它们的用途进行了综述。特别强调了这些新化合物的合成、亲电取代反应以及我们实验室开发的新型合成方法。基于大量报告和现有数据,我们认为DNA嵌入位点和膜相互作用位点是它们发挥作用的靶点。

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