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.

引用

页数：16

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