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The Synthesis, Metal Exchange, and Hyaluronate Functionalization of a Cationic Gallium-Based Thiosemicarbazone Anticancer Drug.

Molecules (Basel, Switzerland) 2026 Vol.31(3)

Ning Y, Dong ML, Zhang WH, Young DJ

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We herein demonstrate that the thiosemicarbazone (TSC) ligand N'-(di(pyridin-2-yl)methylene)-4-(thiazol-2-yl)piperazine-1-carbothiohydrazide (H) can coordinate with Ga to give cationic complex featur

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APA Ning Y, Dong ML, et al. (2026). The Synthesis, Metal Exchange, and Hyaluronate Functionalization of a Cationic Gallium-Based Thiosemicarbazone Anticancer Drug.. Molecules (Basel, Switzerland), 31(3). https://doi.org/10.3390/molecules31030577
MLA Ning Y, et al.. "The Synthesis, Metal Exchange, and Hyaluronate Functionalization of a Cationic Gallium-Based Thiosemicarbazone Anticancer Drug.." Molecules (Basel, Switzerland), vol. 31, no. 3, 2026.
PMID 41683553

Abstract

We herein demonstrate that the thiosemicarbazone (TSC) ligand N'-(di(pyridin-2-yl)methylene)-4-(thiazol-2-yl)piperazine-1-carbothiohydrazide (H) can coordinate with Ga to give cationic complex featuring an octahedral Ga(III) center. undergoes metathesis with both Fe and Fe, resulting in the formation of respective Fe- and Fe complexes. is also susceptible to anion exchange with sodium hyaluronate (NaA) to produce the nanoformulation with boosted aqueous solubility and cell targeting. demonstrated remarkable in vitro cytotoxicity against NCI-H82 and A549 (lung cancer), as well as KYSE-510 and Te-1 (esophageal cancer) cell lines, featuring half maximal inhibitory concentration (IC) values in the range 0.102-2.616 μmol L. This work highlights the potential of using non-toxic and biocompatible Ga as the central ion to prepare TSC-based nanomedicines for combating cancer.

MeSH Terms

Humans; Antineoplastic Agents; Hyaluronic Acid; Thiosemicarbazones; Gallium; Cell Line, Tumor; Cations; Coordination Complexes; Molecular Structure; A549 Cells

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