Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities
Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were scr...
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| Format: | Article |
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MDPI AG
2023-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/23/7912 |
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| author | Maria Karelou Dionysis Kampasis Amalia D. Kalampaliki Leentje Persoons Andreas Krämer Dominique Schols Stefan Knapp Steven De Jonghe Ioannis K. Kostakis |
| author_facet | Maria Karelou Dionysis Kampasis Amalia D. Kalampaliki Leentje Persoons Andreas Krämer Dominique Schols Stefan Knapp Steven De Jonghe Ioannis K. Kostakis |
| author_sort | Maria Karelou |
| collection | DOAJ |
| description | Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were screened for their potency and selectivity against a panel of 109 kinases and four bromodomains, using Differential Scanning Fluorimetry (DSF). Compound <b>17</b> bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines. |
| first_indexed | 2024-03-09T01:46:18Z |
| format | Article |
| id | doaj.art-c1e34cc6d968471da7bd856cf8b08908 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T01:46:18Z |
| publishDate | 2023-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-c1e34cc6d968471da7bd856cf8b089082023-12-08T15:22:44ZengMDPI AGMolecules1420-30492023-12-012823791210.3390/molecules28237912Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative ActivitiesMaria Karelou0Dionysis Kampasis1Amalia D. Kalampaliki2Leentje Persoons3Andreas Krämer4Dominique Schols5Stefan Knapp6Steven De Jonghe7Ioannis K. Kostakis8Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, GreeceDepartment of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, GreeceDepartment of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, GreeceDepartment of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumInstitute for Pharmaceutical Chemistry, Department of Biochemistry, Chemistry and Pharmacy, Goethe University Frankfurt, Max-von-Laue-Straße 9, 60438 Frankfurt, GermanyDepartment of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumInstitute for Pharmaceutical Chemistry, Department of Biochemistry, Chemistry and Pharmacy, Goethe University Frankfurt, Max-von-Laue-Straße 9, 60438 Frankfurt, GermanyDepartment of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, KU Leuven, Herestraat 49, P.O. Box 1043, 3000 Leuven, BelgiumDepartment of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, GreeceSixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were screened for their potency and selectivity against a panel of 109 kinases and four bromodomains, using Differential Scanning Fluorimetry (DSF). Compound <b>17</b> bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines.https://www.mdpi.com/1420-3049/28/23/7912quinazolinessynthesisanti-proliferative activitykinase inhibition |
| spellingShingle | Maria Karelou Dionysis Kampasis Amalia D. Kalampaliki Leentje Persoons Andreas Krämer Dominique Schols Stefan Knapp Steven De Jonghe Ioannis K. Kostakis Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities Molecules quinazolines synthesis anti-proliferative activity kinase inhibition |
| title | Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities |
| title_full | Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities |
| title_fullStr | Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities |
| title_full_unstemmed | Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities |
| title_short | Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities |
| title_sort | synthesis and biological evaluation of 2 substituted quinazolin 4 3 i h i ones with antiproliferative activities |
| topic | quinazolines synthesis anti-proliferative activity kinase inhibition |
| url | https://www.mdpi.com/1420-3049/28/23/7912 |
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