期刊
MOLECULES
卷 27, 期 20, 页码 -出版社
MDPI
DOI: 10.3390/molecules27206977
关键词
thiosemicarbazides; 1; 3; 4-thiadiazoles; anticancer activity; breast cancer; mechanism of action
资金
- Medical University of Lublin, Poland [DS 15]
- Medical University of Bialystok, Poland [SUB/2/DN/21/002/2229]
Based on previous work, we designed and synthesized 1,3,4-thiadiazole derivatives and evaluated their cytotoxic activity against breast cancer cells. The compounds displayed weak anticancer activity, with SCT-4 showing the most significant effect on MCF-7 breast cancer cells. Further investigation suggested a possible multitarget mode of action for the synthesized compounds, with a potential involvement of caspase 8.
Based on the results of previous work, we designed and synthesized 1,3,4-thiadiazole derivatives. The cytotoxic activity of the obtained compounds was then determined in biological studies using MCF-7 and MDA-MB-231 breast cancer cells and a normal cell line (fibroblasts). The results showed that all compounds displayed weak anticancer activity towards two breast cancer lines: an estrogen-dependent cell line (MCF-7) and an estrogen-independent cell line (MDA-MB-231). The compound most active towards MCF-7 breast cancer cells was SCT-4, which decreased DNA biosynthesis to 70% +/- 3 at 100 mu M. The mechanism of the anticancer action of 1,3,4-thiadiazole was also investigated. We choose a set of the most investigated proteins, which are attractive anticancer targets. In silico studies demonstrated a possible multitarget mode of action for the synthesized compounds but the most likely mechanism of action for the new compounds is connected with the activity of caspase 8.
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