Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities
Maria Karelou, Dionysis Kampasis, Amalia D. Kalampaliki, Leentje Persoons, Andreas Krämer, Dominique Schols, Stefan Knapp, Steven De Jonghe, Ioannis K. Kostakis · 2023
Read Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities by Maria Karelou, Dionysis Kampasis, Amalia D. Kalampaliki, Leentje Persoons, Andreas Krämer, Dominique Schols, Stefan Knapp, Steven De Jonghe, Ioannis K. Kostakis (2023) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-10707894.txt.
Description
Maria Karelou and eight colleagues synthesized sixteen new quinazoline compounds and tested them against cancer cells. Quinazolinones are a versatile scaffold in medicinal chemistry. The team built the compounds from simple methoxy-bearing starting acids through a straightforward route. Every compound was screened against nine cancer cell lines. A second screen measured activity and selectivity across 109 kinases and four bromodomains.
One compound stood out sharply. Bearing a methoxyphenyl group and a basic side chain, it showed strong activity against most of the tested cell lines. Thermal shift screening helped show which protein targets the series engages. The twenty twenty-three study narrows a broad chemical family to a promising lead. Follow-up work would need to confirm potency and safety in more detailed models.
Catalog record
| CREATOR | Maria Karelou, Dionysis Kampasis, Amalia D. Kalampaliki, Leentje Persoons, Andreas Krämer, Dominique Schols, Stefan Knapp, Steven De Jonghe, Ioannis K. Kostakis |
|---|---|
| YEAR | 2023 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 47 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |