Synthesis, Stability, and Biological Evaluation of Novel Ami-Noderivatives Incorporating the Aza-Acridine Scaffold
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.
Authors
- Maria Karelou
- Dimitrios J. Stravopodis (ORCID: https://orcid.org/0000-0002-9535-2134)
- Anthi Panara (ORCID: https://orcid.org/0000-0001-9730-6767)
- Aikaterini F. Giannopoulou
- Evagelos Gikas (ORCID: https://orcid.org/0000-0002-0107-9991)
- Ioannis K. Kostakis (ORCID: https://orcid.org/0000-0002-9901-5223)
- Eleftheria Chatziorfanou
Institutions
- National and Kapodistrian University of Athens (GR)
Publication Details
- Journal
- Molecules
- Published
- 2025-06-16
- DOI
- https://doi.org/10.3390/molecules30122612
- Primary Topic
- Cancer therapeutics and mechanisms
- Type
- article
- Field-Weighted Citation Impact
- 0.00