Ufa Institute of Chemistry, Ufa Federal Research Centre of the Russian Academy of Sciences, Ufa, Russian Federation.
Bashkir State Medical University, Ufa, Russian Federation.
Nat Prod Res. 2021 Apr;35(8):1340-1348. doi: 10.1080/14786419.2019.1648459. Epub 2019 Aug 20.
A series of new 1,3-thiazole derivatives of maleopimaric acid , were synthesized and evaluated for anticancer, antibacterial and antifungal activities. Evaluation of cytotoxic activity against human embryonic kidney 293 cells (HEK293), human neuroblastoma cell line (SH-SY5Y), hepatocellular carcinoma cell line (HepG2) and human T-cell lymphoblast-like line (Jurkat), showed that introduction of the aminothiazole fragment at position 6 of the diterpenoid molecule leads to decrease of cell viability. Substance 3 was found to be the most active against all tested cell lines, inhibiting cell viability with IC values in the range of 2-24 μM. The structure-activity relationship of these compounds was studied and the results show that the compounds and exhibited antifungal activity against and also possessed antibacterial profile against , , , , and .
一系列新的马来松香酸 1,3-噻唑衍生物被合成并评估了其抗癌、抗菌和抗真菌活性。对人胚肾 293 细胞（HEK293）、人神经母细胞瘤细胞系（SH-SY5Y）、肝癌细胞系（HepG2）和人 T 细胞淋巴母细胞样系（Jurkat）的细胞毒性活性评估表明，在二萜分子的 6 位引入氨基噻唑片段会导致细胞活力下降。发现物质 3 对所有测试的细胞系最具活性，其 IC 值在 2-24μM 的范围内抑制细胞活力。这些化合物的构效关系研究表明，化合物 和 对 和 具有抗真菌活性，并且对 、 、 、 、 和 具有抗菌特性。
