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设计并合成了新型三甲氧基苯基连接型康普瑞汀类似物，负载在金刚石纳米粒子上，作为改善溶解性和抗增殖活性的面板。

Design and synthesis of new trimethoxylphenyl-linked combretastatin analogues loaded on diamond nanoparticles as a panel for ameliorated solubility and antiproliferative activity.

机构信息

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, Egypt.

Chemistry Department, Faculty of Science, Port Said University, Port Said, Egypt.

出版信息

J Enzyme Inhib Med Chem. 2022 Dec;37(1):2679-2701. doi: 10.1080/14756366.2022.2116016.

DOI:10.1080/14756366.2022.2116016
PMID:36154552
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9518609/
Abstract

A new series of vinyl amide-, imidazolone-, and triazinone-linked combretastatin A-4 analogues have been designed and synthesised. These compounds have been evaluated for their cytotoxic activity against MDA-MB-231 breast cancer cells. The triazinone-linked combretastatin analogues (6 and 12) exhibited the most potent cytotoxic activity, in sub-micromolar concentration compared with combretastatin A-4 as a reference standard. The results of β-tubulin polymerisation inhibition assay appear to correlate well with the ability to inhibit β-tubulin polymerisation. Additionally, these compounds were subjected to biological assays relating to cell cycle aspects and apoptosis induction. In addition, the most potent compound was loaded on PEG-PCL modified diamond nanoparticles (PEG-PCL-NDs) and F4 was picked as the optimum formula. F4 exhibited enhanced solubility and release over the drug suspension. In the comparative cytotoxic activity, PEG-PCL modified F4 was capable of diminishing the IC50 by around 2.89 times for nude F4, while by 3.48 times relative to non-formulated compound .

摘要

设计并合成了一系列新的乙烯基酰胺、咪唑啉酮和三嗪酮连接的康普瑞汀 A-4 类似物。评估了这些化合物对 MDA-MB-231 乳腺癌细胞的细胞毒性活性。与康普瑞汀 A-4 作为参比标准相比，三嗪酮连接的康普瑞汀类似物（6 和 12）在亚微米浓度下表现出最强的细胞毒性活性。β-微管蛋白聚合抑制试验的结果似乎与抑制β-微管蛋白聚合的能力很好地相关。此外，这些化合物还进行了与细胞周期方面和细胞凋亡诱导相关的生物学测定。此外，最有效的化合物被负载到 PEG-PCL 修饰的金刚石纳米颗粒（PEG-PCL-NDs）上，选择 F4 作为最佳配方。F4 表现出增强的溶解度和释放超过药物悬浮液。在比较细胞毒性活性中，PEG-PCL 修饰的 F4 能够使裸 F4 的 IC50 降低约 2.89 倍，而相对于未制剂的化合物 ，则降低了 3.48 倍。

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