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5,6‑diiodo‑1H‑benzotriazole: new TBBt analogue that minutely affects mitochondrial activity

Paprocki, Daniel and Winiewska-Szajewska, Maria and Speina, Elzbieta and Kucharczyk, Roza and Poznański, Jarosław (2021) 5,6‑diiodo‑1H‑benzotriazole: new TBBt analogue that minutely affects mitochondrial activity. Scientific Reports, 11 (23701). ISSN 2045-2322


Official URL: https://www.nature.com/articles/s41598-021-03136-8


4,5,6,7‑Tetrabromo‑1H‑benzotriazole is widely used as the eference ATP‑competitive inhibitor of protein kinase CK2. Herein, we study its new analogs: 5,6‑diiodo‑ and ,6‑diiodo‑4,7‑dibromo‑1H‑ benzotriazole. We used biophysical (MST, ITC) and biochemical (enzymatic assay) methods to describe the interactions of halogenated benzotriazoles with the catalytic subunit of human protein kinase CK2 (hCK2α). To trace the biological activity, we measured their ytotoxicity against four reference cancer cell lines and the effect on the mitochondrial inner membrane potential. The results obtained lead to the conclusion that iodinated compounds are an attractive alternative to brominated ones. One of them retains the cytotoxicity against selected cancer cell lines of the reference TBBt with a smaller side effect on mitochondrial activity. Both iodinated compounds are andidate leaders in the further development of CK2 inhibitors.

Item Type:Article
Subjects:Q Science > QD Chemistry
Divisions:Department of Biophysics
ID Code:2121
Deposited By: Dr Adam Mieczkowski
Deposited On:13 Dec 2021 11:31
Last Modified:13 Dec 2021 11:31

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