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

Institutions

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
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Synthesis, Stability, and Biological Evaluation of Novel Ami-Noderivatives Incorporating the Aza-Acridine Scaffold

Maria Karelou, Dimitrios J. Stravopodis, Anthi Panara, Aikaterini F. Giannopoulou et al.
Molecules
Cancer therapeutics and mechanisms
article

Synthesis, Stability, and Biological Evaluation of Novel Ami-Noderivatives Incorporating the Aza-Acridine Scaffold

Maria Karelou, Dimitrios J. Stravopodis, Anthi Panara, Aikaterini F. Giannopoulou, Evagelos Gikas, Ioannis K. Kostakis, Eleftheria Chatziorfanou
article en

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.

MoleculesVol. 30(12)
National and Kapodistrian University of Athens (GR)
Openalex Percentile: Top 87%
Cancer therapeutics and mechanisms
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.

Synthesis, Stability, and Biological Evaluation of Novel Ami-Noderivatives Incorporating the Aza-Acridine Scaffold — Maria Karelou, Dimitrios J. Stravopodis, et al. · Molecules (2025) | TGRS Research Map | TGRS