Key result
Platinum(II) complex Pt1a exhibits strong cytotoxicity against doxorubicin-resistant colorectal cancer cells at ~0.7 μM.
Why the study?
The growing resistance to conventional chemotherapy in colorectal cancer highlights the need for new therapeutic strategies against drug-resistant CRC.
Effect estimate: IC50 = 0.7 μM
The novel platinum(II) complex Pt1a demonstrates potent cytotoxicity against drug-resistant colorectal cancer cells with favorable mechanistic and safety profiles in preclinical models.
Novel Pt(II) complexes merit evaluation in drug-resistant CRC models; hypothesis-generating and requires validation before clinical consideration.
Colorectal cancer (CRC) remains a major global health burden, with approximately 2 million new cases and 1 million deaths annually. The growing resistance to conventional chemotherapy highlights the need for new therapeutic strategies against drug-resistant CRC. In this study, platinum(II) complexes of the general formula [PtCl(Ln)]CF3SO3, based on substituted 2,2′:6′,2″-terpyridines (Pt1) and 2,6-bis(thiazol-2-yl)pyridines (Pt2), were synthesized and evaluated for anticancer activity. Their antiproliferative effects were assessed in doxorubicin-sensitive and doxorubicin-resistant CRC cell lines, as well as primary dermal fibroblasts. Among the tested complexes, Pt1a showed the highest potency, exhibiting strong cytotoxicity against HCT116-DoxR cells (IC50 = 0.7 μM). Mechanistic studies revealed that Pt1a increases reactive oxygen species levels, binds DNA, disrupts cell cycle progression, and induces apoptosis and autophagy. Pt1a also displayed anti-metastatic and anti-angiogenic activities, showed favourable interaction with bovine serum albumin, and exhibited no detectable toxicity in a chicken embryo model.
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Maroń et al. (2026) studied Colorectal cancer. Platinum(II) complexes (Pt1a) was evaluated on Cytotoxicity against HCT116-DoxR cells (IC50 = 0.7 μM). The platinum(II) complex Pt1a exhibited strong cytotoxicity against doxorubicin-resistant colorectal cancer cells (IC50 = 0.7 μM) and showed no detectable toxicity in a chicken embryo model.
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