Data · dataset · 2026
Promising Anticancer Prodrugs Based on Pt(IV) Complexes with Bisorganosilane Ligands in Axial Positions
Listed in e-cienciaDatos
We report two novel prodrug Pt(IV) complexes with bis-organosilane ligands in axial positions: cis-dichloro(diamine)-trans-[3-(triethoxysilyl)propylcarbamate]-platinum(IV) (Pt(IV)-biSi-1) and cis-dichloro(diisopropylamine)-trans-[3-(triethoxysilyl)propyl carbamate]platinum(IV) (Pt(IV)-biSi-2).
Description
Pt(IV)-biSi-2 demonstrated enhanced in vitro cytotoxicity against colon cancer cells (HCT 116 and HT-29) compared with cisplatin and Pt(IV)-biSi-1.
Notably, Pt(IV)-biSi-2 exhibited higher cytotoxicity toward cancer cells and lower toxicity on nontumorigenic intestinal cells (HIEC6). In preclinical mouse models of colorectal cancer, Pt(IV)-biSi-2 outperformed cisplatin in reducing tumor growth at lower concentrations, with reduced side effects. Mechanistically, Pt(IV)-biSi-2 induced permanent DNA damage independent of p53 levels.
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DNA damage such as double-strand breaks marked by histone gH2Ax was permanent after treatment with Pt(IV)-biSi-2, in contrast to cisplatin's transient effects. Pt(IV)-biSi-2's faster reduction to Pt(II) species upon exposure to biological reductants supports its superior biological response. These findings unveil a novel strategy for designing Pt(IV) anticancer prodrugs with enhanced activity and specificity, offering therapeutic opportunities beyond conventional Pt drugs.
Links
Where it is published
- Dataverse dataset page edatos.consorciomadrono.es/dataset.xhtml?persistentId=doi%3A10.21950%2F3DUJPM ↗
landing page · from edatos consorciomadrono es
- DOI doi.org/10.21950/3dujpm ↗
DOI / persistent id · from edatos consorciomadrono es
Catalogue records · 1
- Dataverse API edatos.consorciomadrono.es/api/datasets/:persistentId/?persistentId=doi%3A10.21950%2F3DUJ… ↗
metadata API · from edatos consorciomadrono es
Topics
- Stated by source
- Química
- Inferred from text
- Cancer 75% · Inorganic chemistry 72%
Provenance · 1 source records, 9 field assertions
| Source | Key | Last seen | Raw |
|---|---|---|---|
| e-cienciaDatos | doi:10.21950/3DUJPM | 12 d ago | JSON v1 |
| Field | Assertion | Extractor | Evidence |
|---|---|---|---|
| concepts[disease].local:disease:cancer | enrichment · edatos consorciomadrono es | keyword-concept-rules@1.0.0 | title+description (75%) |
| concepts[field].anzsrc:group:3402 | enrichment · edatos consorciomadrono es | taxonomy-embedding@1.1.0 | title+keywords+description (72%) |
| concepts[field].dataverse_subject:qu-mica | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 | /subjects |
| created_date | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 | |
| description | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 | /description |
| publication_date | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 | |
| title | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 | /name |
| updated_date | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 | |
| version_label | source · edatos consorciomadrono es | connector:edatos_consorciomadrono_es@1.0.0 |