Exploring the Impact of Carboxylic Groups on the Anti‐Proliferative Activity of 5‐Aminosalicylic‐4‐Thiazolinone Hybrids: Design, Synthesis, Biological Evaluation, and ADME Study
values of 4.74 µM and 7.16 µM, The overall results show that the methyl ester derivative of the hybrids is the most active among the tested derivatives against all tested cell lines with low micromolar to nanomolar potency. While hybrids with free or amidated carboxylic groups are much less potent. ADME study revealed that the difference in physicochemical properties might rationalize the activity pattern. This study demonstrates that the nature of the carboxylic group in these hybrids critically influences their antiproliferative activity. The findings pave the way for developing optimized anticancer salicylate drugs by focusing on modifications that improve key physicochemical properties.
Authors
- Raafat El‐Awady (ORCID: https://orcid.org/0000-0002-7046-8587)
- Wafaa S. Ramadan (ORCID: https://orcid.org/0000-0002-7334-3093)
- Hajjaj H.M. Abdu-Allah (ORCID: https://orcid.org/0000-0002-4474-9086)
- Varsha Menon
- Shimaa A. Othman
- Abdel‐Nasser A. El‐Shorbagi
Institutions
- University of Sharjah (AE)
- Assiut University (EG)
Publication Details
- Journal
- Chemistry & Biodiversity
- Published
- 2026-04-01
- DOI
- https://doi.org/10.1002/cbdv.202503599
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.00