Design, synthesis, biological assessment, and <i>in silico</i> analysis of bisthiazolidine amide derivatives as potential anti-bacterial and anti-prostate cancer agents

A series of N,N'-(1,4-phenylene) bis(3-acetyl-2-arylthiazolidine-4-carboxamide) derivatives (M1-M5) was synthesized, characterized, and evaluated for antibacterial and anticancer activities. Literature from 2000 to 2023 was reviewed using PubMed and Scopus to guide compound selection. Structural characterization was confirmed via FT-IR, ¹H, ¹³C-NMR, and mass spectrometry. Antibacterial activity was assessed using the disk diffusion method against S. aureus, E. coli, and S. mutans, with M4, M5, and M3 surpassing cefixime, exhibiting MIC values of 9.7, 39.5, and 79 µg/ML against S. aureus. M3 and M5 also showed notable activity against S. mutans. MTT assays revealed potent cytotoxicity of M4, M5, and M3 against PC3 cells, with M4 (IC50 = 19.56 µg/ML) outperforming Darolutamide drug (IC50 = 52.82 µg/ML). Molecular docking suggested EGFR inhibition. M4 induced apoptosis and G1 phase arrest in PC3 cells, demonstrating its potential as a dual-purpose therapeutic agent.

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Publication Details

Journal
Green Chemistry Letters and Reviews
Published
2025-08-14
DOI
https://doi.org/10.1080/17518253.2025.2541058
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.00

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article

Design, synthesis, biological assessment, and in silico analysis of bisthiazolidine amide derivatives as potential anti-bacterial and anti-prostate cancer agents

Mohammad Y. Alfaifi, Serag Eldin I. Elbehairi, Ahmed Y. Hammood, Mohammed Aufy et al.
1 links
Green Chemistry Letters and Reviews
Synthesis and biological activity
article

Design, synthesis, biological assessment, and in silico analysis of bisthiazolidine amide derivatives as potential anti-bacterial and anti-prostate cancer agents

Mohammad Y. Alfaifi, Serag Eldin I. Elbehairi, Ahmed Y. Hammood, Mohammed Aufy, Rehab G. Abood, Ahmed A. Majed, Naser A Naser, Dunya AL-Duhaidahawi, Ali A. Shati, Ahmed Hussein, Sabah Abbas, Huda H. Nameh, Radwan Alanjjar
article en

Abstract

A series of N,N'-(1,4-phenylene) bis(3-acetyl-2-arylthiazolidine-4-carboxamide) derivatives (M1-M5) was synthesized, characterized, and evaluated for antibacterial and anticancer activities. Literature from 2000 to 2023 was reviewed using PubMed and Scopus to guide compound selection. Structural characterization was confirmed via FT-IR, ¹H, ¹³C-NMR, and mass spectrometry. Antibacterial activity was assessed using the disk diffusion method against S. aureus, E. coli, and S. mutans, with M4, M5, and M3 surpassing cefixime, exhibiting MIC values of 9.7, 39.5, and 79 µg/ML against S. aureus. M3 and M5 also showed notable activity against S. mutans. MTT assays revealed potent cytotoxicity of M4, M5, and M3 against PC3 cells, with M4 (IC50 = 19.56 µg/ML) outperforming Darolutamide drug (IC50 = 52.82 µg/ML). Molecular docking suggested EGFR inhibition. M4 induced apoptosis and G1 phase arrest in PC3 cells, demonstrating its potential as a dual-purpose therapeutic agent.

Green Chemistry Letters and ReviewsVol. 18(1)
University of Basrah (IQ), University of Vienna (AT), Girls Incorporated (US), University of Babylon (IQ), Hill College (US), Libyan International Medical University (LY), Institute of Pharmacology (CZ), University of Kufa (IQ), King Khalid University (SA)
King Khalid University
Openalex Percentile: Top 84%
Synthesis and biological activity
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