Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents
Molecular hybridization has become a leading and highly effective method for creating new anticancer chemotherapeutic drugs. In this endeavor, new cyanoacrylamides with derivatives of sulphamethoxazole (5a-5f) have been created and verified utilizing different spectral instruments. The SRB assay eva...
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| Format: | Article |
| Language: | English |
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Elsevier
2025-03-01
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| Series: | Results in Chemistry |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S221171562500102X |
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| author | Fatma G. Mohamed Mohamed A. Ragheb Ahmed H.M. Elwahy Hadeer M. Diab Marwan Emara Mostafa E. Salem Ibrahim O. Althobaiti Ismail A. Abdelhamid |
| author_facet | Fatma G. Mohamed Mohamed A. Ragheb Ahmed H.M. Elwahy Hadeer M. Diab Marwan Emara Mostafa E. Salem Ibrahim O. Althobaiti Ismail A. Abdelhamid |
| author_sort | Fatma G. Mohamed |
| collection | DOAJ |
| description | Molecular hybridization has become a leading and highly effective method for creating new anticancer chemotherapeutic drugs. In this endeavor, new cyanoacrylamides with derivatives of sulphamethoxazole (5a-5f) have been created and verified utilizing different spectral instruments. The SRB assay evaluated the cytotoxic activities of the tested compounds against 16Lu, a human normal cell, and several human cancer cells (HCT116, MCF7, and HepG2). Among all derivatives, 5a and 5b had the most potent cytotoxicity effect against HepG2 cells with IC50 = 11.06 ± 0.829 and 18.836 ± 2.68 μg/ml, respectively. The binding affinities of 5a and 5b with DNA and BSA were studied using different spectroscopic techniques. Furthermore, molecular docking for 5a and 5b was performed to confirm the experimental results and anticipate their binding capabilities toward DNA and BSA. Thus, this work introduces promising antitumor lead compounds, encouraging further activity enhancement and therapeutic development studies. |
| format | Article |
| id | doaj-art-43614295042c46fda6c5df28e2d4e17c |
| institution | DOAJ |
| issn | 2211-7156 |
| language | English |
| publishDate | 2025-03-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Results in Chemistry |
| spelling | doaj-art-43614295042c46fda6c5df28e2d4e17c2025-08-20T02:47:39ZengElsevierResults in Chemistry2211-71562025-03-011410211910.1016/j.rechem.2025.102119Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agentsFatma G. Mohamed0Mohamed A. Ragheb1Ahmed H.M. Elwahy2Hadeer M. Diab3Marwan Emara4Mostafa E. Salem5Ibrahim O. Althobaiti6Ismail A. Abdelhamid7Chemistry Department (Biochemistry Division), Faculty of Science, Cairo University, Giza P.O. 12613, EgyptChemistry Department (Biochemistry Division), Faculty of Science, Cairo University, Giza P.O. 12613, Egypt; Biotechnology Department, Faculty of Nanotechnology for Postgraduate Studies, Cairo University, Sheikh Zayed Branch Campus, Giza 12588, EgyptChemistry Department, Faculty of Science, Cairo University, Giza P.O. 12613, Egypt; Corresponding authors.Chemistry Department, Faculty of Science, Cairo University, Giza P.O. 12613, EgyptCenter for Aging and Associated Diseases, Zewail City of Science, Technology and Innovation, 12578 Giza, EgyptCollege of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), P.O. Box, 90950, Riyadh 11623, Saudi ArabiaDepartment of Chemistry, Faculty of Science, Islamic University of Madinah, Madinah 42351, Saudi ArabiaChemistry Department, Faculty of Science, Cairo University, Giza P.O. 12613, Egypt; Corresponding authors.Molecular hybridization has become a leading and highly effective method for creating new anticancer chemotherapeutic drugs. In this endeavor, new cyanoacrylamides with derivatives of sulphamethoxazole (5a-5f) have been created and verified utilizing different spectral instruments. The SRB assay evaluated the cytotoxic activities of the tested compounds against 16Lu, a human normal cell, and several human cancer cells (HCT116, MCF7, and HepG2). Among all derivatives, 5a and 5b had the most potent cytotoxicity effect against HepG2 cells with IC50 = 11.06 ± 0.829 and 18.836 ± 2.68 μg/ml, respectively. The binding affinities of 5a and 5b with DNA and BSA were studied using different spectroscopic techniques. Furthermore, molecular docking for 5a and 5b was performed to confirm the experimental results and anticipate their binding capabilities toward DNA and BSA. Thus, this work introduces promising antitumor lead compounds, encouraging further activity enhancement and therapeutic development studies.http://www.sciencedirect.com/science/article/pii/S221171562500102XCyanoacrylamidesAnticancer activityDNA and BSA binding affinitiesDocking |
| spellingShingle | Fatma G. Mohamed Mohamed A. Ragheb Ahmed H.M. Elwahy Hadeer M. Diab Marwan Emara Mostafa E. Salem Ibrahim O. Althobaiti Ismail A. Abdelhamid Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents Results in Chemistry Cyanoacrylamides Anticancer activity DNA and BSA binding affinities Docking |
| title | Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents |
| title_full | Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents |
| title_fullStr | Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents |
| title_full_unstemmed | Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents |
| title_short | Synthesis, cytotoxic evaluation, and binding studies of novel sulphamethoxazole-based cyanoacrylamides as potential antitumor agents |
| title_sort | synthesis cytotoxic evaluation and binding studies of novel sulphamethoxazole based cyanoacrylamides as potential antitumor agents |
| topic | Cyanoacrylamides Anticancer activity DNA and BSA binding affinities Docking |
| url | http://www.sciencedirect.com/science/article/pii/S221171562500102X |
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