What question did this study set out to answer?

To evaluate the Topo IIα inhibitory activity and anticancer mechanisms of novel bis-thiourea derivatives.

August 15, 2026ACS OmegaOpen Access

Discovery of Bis-ThioureaDerivatives as Human DNATopoisomerase IIα Inhibitors with Potent Anticancer Effects

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In vitro study demonstrates bis-thiourea derivative inhibition of Topo IIα and cancer invasion, indicating potential for targeted cancer therapy.

To evaluate the Topo IIα inhibitory activity and anticancer mechanisms of novel bis-thiourea derivatives.
Performed in silico molecular modeling to determine compound binding affinity and stability in the Topo IIα ATPase domain.
Conducted in vitro biochemical assays to measure Topo IIα inhibition, cytotoxicity, cell migration, invasion, and cell-cycle distribution across cancer cell lines, including A549.
Compound 8 docked stably in the ATPase domain of Topo IIα, inhibited enzyme activity, and exhibited potent cytotoxicity, especially in A549 cells.
Compound 8 suppressed A549 cell migration and invasion by increasing E-cadherin expression and reducing N-cadherin, vimentin, and Slug levels.
Compound 8 induced G1-phase cell-cycle arrest through downregulation of cyclins D1 and E2 alongside upregulation of p21.

Sabuakham et al. (2026) studied this question.

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In vitro study demonstrates bis-thiourea derivative inhibition of Topo IIα and cancer invasion, indicating potential for targeted cancer therapy.