Department of Inorganic and Analytical Chemistry, Nicolaus Copernicus University in Toruń, Ludwik Rydygier Collegium Medicum in Bydgoszcz, 85-089 Bydgoszcz, Poland.
Int J Mol Sci. 2019 Mar 14;20(6):1300. doi: 10.3390/ijms20061300.
The growing interest in anticancer hybrids in the last few years has resulted in a great number of reports on hybrid design, synthesis and bioevaluation. Many novel multi-target-directed drug candidates were synthesized, and their biological activities were evaluated. For the design of anticancer hybrid compounds, the molecules of stilbenes, aromatic quinones, and heterocycles (benzimidazole, imidazole, pyrimidine, pyridine, pyrazole, quinoline, quinazoline) were applied. A distinct group of hybrids comprises the molecules built with natural compounds: Resveratrol, curcumin, coumarin, and oleanolic acid. In this review, we present the studies on bioactive hybrid molecules of a well-known tubulin polymerization inhibitor, combretastatin A-4 and its analogs with other pharmacologically active entities. The mechanism of anticancer activity of selected hybrids is discussed considering the structure-activity relationship.
近年来，人们对抗癌杂合子越来越感兴趣，导致大量关于杂合子设计、合成和生物评价的报告。许多新型多靶点导向药物候选物被合成，并对其生物活性进行了评估。在抗癌杂合化合物的设计中，应用了二苯乙烯类、芳基醌类和杂环（苯并咪唑、咪唑、嘧啶、吡啶、吡唑、喹啉、喹唑啉）类分子。一类明显的杂合物包括与天然化合物构建的分子：白藜芦醇、姜黄素、香豆素和齐墩果酸。在这篇综述中，我们介绍了具有良好的微管聚合抑制剂活性的化合物，如 combretastatin A-4 及其与其他具有药理活性的化合物的生物活性杂合分子的研究。考虑到结构-活性关系，讨论了所选杂合物的抗癌活性机制。
