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评估查尔酮酞菁缀合物的双重活性:设计、合成及抗血管生成和光动力特性。

Assessing the dual activity of a chalcone-phthalocyanine conjugate: design, synthesis, and antivascular and photodynamic properties.

机构信息

Department of Chemistry, Gebze Institute of Technology , P.O. Box 141, 41400 Gebze, Kocaeli, Turkey.

出版信息

Mol Pharm. 2013 Oct 7;10(10):3706-16. doi: 10.1021/mp400207v. Epub 2013 Sep 3.

Abstract

Photodynamic therapy (PDT) and vascular-disrupting agents (VDA) each have their advantages in the treatment of solid tumors, but also present drawbacks. In PDT, hypoxia at the center of the tumor limits conversion of molecular oxygen into singlet oxygen, while VDAs are deficient at affecting the rim of the tumor. A phthalocyanine-chalcone conjugate combining the VDA properties of chalcones with the PDT properties of phthalocyanines was designed to address these deficiencies. Its vascular targeting, photophysical, photochemical, photodynamic activities are reported herein.

摘要

光动力疗法 (PDT) 和血管破坏剂 (VDA) 在治疗实体瘤方面各有优势,但也存在缺点。在 PDT 中,肿瘤中心的缺氧限制了分子氧转化为单线态氧,而 VDAs 则缺乏对肿瘤边缘的影响。本文设计了一种酞菁-查耳酮缀合物,将查耳酮的 VDA 性质与酞菁的 PDT 性质结合在一起,以解决这些不足。本文报道了其血管靶向性、光物理、光化学和光动力活性。

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