Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents
In the present study, a set of 2-anilino-4-alkylaminoquinazoline derivatives were synthesized and tested for their antitumor activities in vitro against a panel of four human cancer cell lines and for their DNA-binding affinity. Among the synthesized compounds, 4c and 5b with 4-substitution at the p...
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| Format: | Article |
| Language: | English |
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Wiley
2022-01-01
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| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2022/7763545 |
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| _version_ | 1832569196326682624 |
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| author | Mohammad A. Alassaf Khalid B. Selim Magda N. A. Nasr |
| author_facet | Mohammad A. Alassaf Khalid B. Selim Magda N. A. Nasr |
| author_sort | Mohammad A. Alassaf |
| collection | DOAJ |
| description | In the present study, a set of 2-anilino-4-alkylaminoquinazoline derivatives were synthesized and tested for their antitumor activities in vitro against a panel of four human cancer cell lines and for their DNA-binding affinity. Among the synthesized compounds, 4c and 5b with 4-substitution at the phenyl ring were found to have the highest inhibitory effects against breast adenocarcinoma (MCF-7), colon cancer (HCT-116), hepatocellular carcinoma (HePG-2), and human skin cancer (HFB4). Further investigation revealed that compounds 4a and 5d exhibited better affinity to bind with DNA than other tested compounds. |
| format | Article |
| id | doaj-art-757dc1a8afb54c519a636c6738741d44 |
| institution | Kabale University |
| issn | 2090-9071 |
| language | English |
| publishDate | 2022-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-757dc1a8afb54c519a636c6738741d442025-02-02T23:03:19ZengWileyJournal of Chemistry2090-90712022-01-01202210.1155/2022/7763545Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor AgentsMohammad A. Alassaf0Khalid B. Selim1Magda N. A. Nasr2Department of Pharmaceutical Organic ChemistryDepartment of Pharmaceutical Organic ChemistryDepartment of Pharmaceutical Organic ChemistryIn the present study, a set of 2-anilino-4-alkylaminoquinazoline derivatives were synthesized and tested for their antitumor activities in vitro against a panel of four human cancer cell lines and for their DNA-binding affinity. Among the synthesized compounds, 4c and 5b with 4-substitution at the phenyl ring were found to have the highest inhibitory effects against breast adenocarcinoma (MCF-7), colon cancer (HCT-116), hepatocellular carcinoma (HePG-2), and human skin cancer (HFB4). Further investigation revealed that compounds 4a and 5d exhibited better affinity to bind with DNA than other tested compounds.http://dx.doi.org/10.1155/2022/7763545 |
| spellingShingle | Mohammad A. Alassaf Khalid B. Selim Magda N. A. Nasr Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents Journal of Chemistry |
| title | Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents |
| title_full | Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents |
| title_fullStr | Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents |
| title_full_unstemmed | Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents |
| title_short | Synthesis and Biological Evaluation of 2,4-Diaminoquinazolines as Potential Antitumor Agents |
| title_sort | synthesis and biological evaluation of 2 4 diaminoquinazolines as potential antitumor agents |
| url | http://dx.doi.org/10.1155/2022/7763545 |
| work_keys_str_mv | AT mohammadaalassaf synthesisandbiologicalevaluationof24diaminoquinazolinesaspotentialantitumoragents AT khalidbselim synthesisandbiologicalevaluationof24diaminoquinazolinesaspotentialantitumoragents AT magdananasr synthesisandbiologicalevaluationof24diaminoquinazolinesaspotentialantitumoragents |