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新型 4-(3,4,5-三甲氧基苯基)噻唑-嘧啶衍生物的设计与合成及其作为潜在的抗增殖剂。

Design and Synthesis of New 4-(3,4,5-Trimethoxyphenyl)Thiazole-Pyrimidine Derivatives as Potential Antiproliferative Agents.

机构信息

Center for Brain Technology, Brain Science Institute, Korea Institute of Science and Technology (KIST), Seoul 02792, Republic of Korea.

Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.

出版信息

Medicina (Kaunas). 2023 Jun 2;59(6):1076. doi: 10.3390/medicina59061076.

DOI:10.3390/medicina59061076
PMID:37374282
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10303439/
Abstract

A new series of 3,4,5-trimethoxyphenyl thiazole pyrimidines has been synthesized and biologically evaluated for its in vitro anticancer activity. Compounds , , and with substituted piperazine showed the best antiproliferative activity. In the NCI-60 cell line screening, compound showed promising cytostatic activity against multiple cell lines. Notably, it elicited a GI value of 86.28% against the NSCL cancer cell line HOP-92 at a 10 μM dose. Compounds and at 10 μM showed promising GI values of 40.87% and 46.14% against HCT-116 colorectal carcinoma and SK-BR-3 breast cancer cell lines, respectively. ADME-Tox prediction of compounds , and revealed their acceptable drug-likeness properties. In addition, compounds , , and showed a high probability of targeting kinase receptors via Molinspiration and Swiss TargetPrediction.

摘要

已合成了一系列新的 3,4,5-三甲氧基苯基噻唑嘧啶，并对其体外抗癌活性进行了生物评价。带有取代哌嗪的化合物 、 和 表现出最佳的增殖抑制活性。在 NCI-60 细胞系筛选中，化合物 对多种细胞系表现出有前途的细胞生长抑制活性。值得注意的是，它在 10 μM 剂量下对 NSCLC 癌细胞系 HOP-92 产生了 86.28%的 GI 值。化合物 和 在 10 μM 时对 HCT-116 结肠直肠癌细胞系和 SK-BR-3 乳腺癌细胞系分别表现出有前途的 GI 值 40.87%和 46.14%。化合物 、 和 的 ADME-Tox 预测表明它们具有可接受的类药性。此外，化合物 、 、 和 通过 Molinspiration 和 Swiss TargetPrediction 显示出靶向激酶受体的高概率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/1abc80d4b194/medicina-59-01076-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/c9da16b289d1/medicina-59-01076-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/52766338d770/medicina-59-01076-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/67e0b2d2f4a7/medicina-59-01076-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/965c603d7c2f/medicina-59-01076-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/1abc80d4b194/medicina-59-01076-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/c9da16b289d1/medicina-59-01076-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/52766338d770/medicina-59-01076-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/67e0b2d2f4a7/medicina-59-01076-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/965c603d7c2f/medicina-59-01076-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a9c/10303439/1abc80d4b194/medicina-59-01076-g003.jpg

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