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评估新型合成噻唑衍生物作为潜在的芳香酶抑制剂对乳腺癌的作用。

Evaluation of novel synthesized thiazole derivatives as potential aromatase inhibitors against breast cancer.

机构信息

Department of Biotechnology, College of Sciences, Taif University, PO Box 11099, Taif, 21944, Saudi Arabia.

Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, PO Box 84428, Riyadh, 11671, Saudi Arabia.

出版信息

Future Med Chem. 2024;16(8):707-721. doi: 10.4155/fmc-2023-0323. Epub 2024 Mar 15.

Abstract

4-Methylacetophenone is used in the preparation of starting materials, 4-methylphenacyle bromide () and 4-methylacetophenone thiosemicarbazole (). Several novel 2,4-disubstituted-1,3-thiazole analogues were obtained via the treatment of starting materials with 4-methylphenacyl bromide, acetyl chloride, aromatic aldehydes and bromination providing thiazole derivatives respectively. Compounds were investigated for their cytotoxic activity on MCF-7 and normal breast cells. Active compounds were found and in contrast to staurosporine, compound displayed the most potent cytotoxic action that showed a strong inhibitory effect (aromatase) and (protein tyrosine kinase) enzymes, proving that the novel thiazole derivatives promoted the effective anticancer drug candidates.

摘要

4-甲基苯乙酮用于制备起始原料,4-甲基苯甲酰溴()和 4-甲基苯乙酮噻唑()。通过用 4-甲基苯甲酰溴、乙酰氯、芳醛和溴化处理起始原料,得到了几种新型 2,4-二取代-1,3-噻唑类似物。将化合物用于 MCF-7 和正常乳腺细胞的细胞毒性活性研究。发现了活性化合物,与星形孢菌素相反,化合物表现出最强的细胞毒性作用,显示出强烈的抑制作用(芳香酶)和(蛋白酪氨酸激酶)酶,证明新型噻唑衍生物促进了有效的抗癌候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7dce/11221541/ee21b97c83c8/IFMC_A_2340290_UF0001_C.jpg

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