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.

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Journal
Chemistry & Biodiversity
Published
2026-04-01
DOI
https://doi.org/10.1002/cbdv.202503599
Primary Topic
Synthesis and biological activity
Type
article
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article

Exploring the Impact of Carboxylic Groups on the Anti‐Proliferative Activity of 5‐Aminosalicylic‐4‐Thiazolinone Hybrids: Design, Synthesis, Biological Evaluation, and ADME Study

Raafat El‐Awady, Wafaa S. Ramadan, Hajjaj H.M. Abdu-Allah, Varsha Menon et al.
Chemistry & Biodiversity
Synthesis and biological activity
article

Exploring the Impact of Carboxylic Groups on the Anti‐Proliferative Activity of 5‐Aminosalicylic‐4‐Thiazolinone Hybrids: Design, Synthesis, Biological Evaluation, and ADME Study

Raafat El‐Awady, Wafaa S. Ramadan, Hajjaj H.M. Abdu-Allah, Varsha Menon, Shimaa A. Othman, Abdel‐Nasser A. El‐Shorbagi
article en

Abstract

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.

Chemistry & BiodiversityVol. 23(4)
University of Sharjah (AE), Assiut University (EG)
Openalex Percentile: Top 22%
Synthesis and biological activity
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