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新型噻唑类查耳酮作为微管蛋白聚合抑制剂的合成及其潜在抗癌活性研究

Synthesis of New Thiazole-Privileged Chalcones as Tubulin Polymerization Inhibitors with Potential Anticancer Activities.

作者信息

Hashem Hamada, Hassan Abdelfattah, Abdelmagid Walid M, Habib Ahmed G K, Abdel-Aal Mohamed A A, Elshamsy Ali M, El Zawily Amr, Radwan Ibrahim Taha, Bräse Stefan, Abdel-Samea Ahmed S, Rabea Safwat M

机构信息

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Sohag University, Sohag 82524, Egypt.

Medicinal Chemistry Department, Faculty of Pharmacy, South Valley University, Qena 52242, Egypt.

出版信息

Pharmaceuticals (Basel). 2024 Aug 31;17(9):1154. doi: 10.3390/ph17091154.

DOI:10.3390/ph17091154
PMID:39338317
原文链接:
https://pmc.ncbi.nlm.nih.gov/articles/PMC11435058/
Abstract

A series of novel thiazole-based chalcones were evaluated for their anticancer activity as potential tubulin polymerization inhibitors. In vitro anticancer screening for the thiazole derivatives - exhibited broad-spectrum antitumor activity against various cancer cell lines particularly Ovar-3 and MDA-MB-468 cells with a GI range from 1.55 to 2.95 μΜ, respectively. Compound demonstrated significant inhibition of tubulin polymerization, with an IC value of 7.78 μM compared to Combretastatin-A4 (CA-4), with an IC value of 4.93 μM. Molecular docking studies of compounds , , and into tubulin further supported these findings, revealing that they bind effectively to the colchicine binding site, mirroring key interactions exhibited by CA-4. Computational predictions suggested favorable oral bioavailability and drug-likeness for these compounds, highlighting their potential for further development as chemotherapeutic agents.

摘要

评估了一系列新型噻唑基查耳酮作为潜在微管蛋白聚合抑制剂的抗癌活性。对噻唑衍生物进行的体外抗癌筛选显示，其对各种癌细胞系具有广谱抗肿瘤活性，特别是对Ovar-3和MDA-MB-468细胞，其GI值分别为1.55至2.95μM。化合物表现出对微管蛋白聚合的显著抑制作用，IC值为7.78μM，而康普瑞他汀-A4（CA-4）的IC值为4.93μM。化合物、和与微管蛋白的分子对接研究进一步支持了这些发现，表明它们能有效结合到秋水仙碱结合位点，反映出CA-4所表现出的关键相互作用。计算预测表明这些化合物具有良好的口服生物利用度和类药性质，突出了它们作为化疗药物进一步开发的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/cc85230ec328/pharmaceuticals-17-01154-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/86ac05400269/pharmaceuticals-17-01154-g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/cc85230ec328/pharmaceuticals-17-01154-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/1282be822915/pharmaceuticals-17-01154-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/385a30b7d8d8/pharmaceuticals-17-01154-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/2417f1fbce97/pharmaceuticals-17-01154-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/80054c2c66e2/pharmaceuticals-17-01154-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/760c1df72dbf/pharmaceuticals-17-01154-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/461d67effca0/pharmaceuticals-17-01154-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/be260fa9d348/pharmaceuticals-17-01154-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/86ac05400269/pharmaceuticals-17-01154-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/c9dc7a4d175c/pharmaceuticals-17-01154-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/a1613fc7ca42/pharmaceuticals-17-01154-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/07a0ed6cfb1d/pharmaceuticals-17-01154-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35fc/11435058/cc85230ec328/pharmaceuticals-17-01154-g011.jpg

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