Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities

被引：3
作者：
Karelou, Maria [1 ]
Kampasis, Dionysis [1 ]
Kalampaliki, Amalia D. [1 ]
Persoons, Leentje [2 ]
Kraemer, Andreas [3 ,4 ]
Schols, Dominique [2 ]
Knapp, Stefan [3 ,4 ]
De Jonghe, Steven [2 ]
Kostakis, Ioannis K. [1 ]
Nikolaropoulos, Sotiris S.
机构：
[1] Natl & Kapodistrian Univ Athens, Dept Pharm, Div Pharmaceut Chem, Athens 15771, Greece
[2] Katholieke Univ Leuven, Rega Inst Med Res, Dept Microbiol Immunol & Transplantat, Lab Virol & Chemotherapy, Herestraat 49, 3000 Leuven, B-1043 Leuven, Belgium
[3] Goethe Univ Frankfurt, Inst Pharmaceut Chem, Dept Biochem Chem & Pharm, Max von Laue Str 9, D-60438 Frankfurt, Germany
[4] Goethe Univ Frankfurt, Buchmann Inst Mol Life Sci, Struct Genom Consortium, Max von Laue Str 15, D-60438 Frankfurt, Germany
来源：
MOLECULES | 2023年 / 28卷 / 23期
关键词：
quinazolines; synthesis; anti-proliferative activity; kinase inhibition; DESIGN;
D O I：
10.3390/molecules28237912
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 17 bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines.
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页数：16
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