# Synthesis, Stability, and Biological Evaluation of Novel Aminoderivatives Incorporating the Aza-Acridine Scaffold

**Authors:** Maria Karelou, Anthi Panara, Eleftheria Chatziorfanou, Aikaterini F. Giannopoulou, Dimitrios J. Stravopodis, Evagelos Gikas, Ioannis K. Kostakis

PMC · DOI: 10.3390/molecules30122612 · Molecules · 2025-06-16

## TL;DR

Researchers designed and tested new aza-acridine compounds with anticancer properties, showing better effectiveness in some cancer cell types and good stability.

## Contribution

The paper introduces novel aza-acridine derivatives with enhanced anticancer activity and stability.

## Key findings

- Some compounds showed significant antiproliferative effects, especially in WM266-4 melanoma cells.
- The most active compounds were stable under aqueous conditions, supported by computational analysis.
- Cell-type selectivity may be due to differences in mutational profiles and molecular targets.

## Abstract

Several new amino-substituted aza-acridine derivatives bearing one or two basic side chains have been designed and synthesized. Their anticancer activities were evaluated in vitro against two human cancer cell lines: T24 (urothelial bladder carcinoma, malignancy grade III) and WM266-4 (metastatic melanoma). Some of the synthesized compounds induced significant antiproliferative effects, with WM266-4 cells appearing more susceptible than T24 cells. This apparent cell-type selectivity may reflect differences in the mutational profiles and molecular target landscapes between the two cancer models. A stability study under hydrolytic conditions, based on a validated method, indicated that the most active compounds were stable under aqueous conditions. Computational analysis further supported the stability of these analogs, providing insights into the structure–stability relationships of the synthesized compounds.

## Linked entities

- **Chemicals:** aza-acridine (PubChem CID 193288)
- **Diseases:** metastatic melanoma (MONDO:0005191)
- **Species:** Homo sapiens (taxon 9606)

## Full-text entities

- **Diseases:** metastatic melanoma (MESH:D008545), cancer (MESH:D009369), urothelial bladder carcinoma (MESH:D001749)
- **Chemicals:** Aza-Acridine (-)
- **Species:** Homo sapiens (human, species) [taxon 9606]
- **Cell lines:** WM266-4 — Homo sapiens (Human), Melanoma, Cancer cell line (CVCL_2765), T24 — Homo sapiens (Human), Bladder carcinoma, Cancer cell line (CVCL_0554)

## Full text

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## Figures

8 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12195947/full.md

## References

42 references — full list in the complete paper: https://tomesphere.com/paper/PMC12195947/full.md

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Source: https://tomesphere.com/paper/PMC12195947