Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities-Reference-Cited by-同舟云学术

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

Published:2023-12-02 Issue:23 Volume:28 Page:7912
ISSN:1420-3049
Container-title:Molecules
language:en
Short-container-title:Molecules

Author:

Karelou Maria¹,Kampasis Dionysis¹^ORCID,Kalampaliki Amalia D.¹^ORCID,Persoons Leentje²^ORCID,Krämer Andreas³⁴,Schols Dominique²^ORCID,Knapp Stefan³⁴^ORCID,De Jonghe Steven²^ORCID,Kostakis Ioannis K.¹^ORCID

Affiliation:

1. Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece

2. Department 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, Belgium

3. Institute for Pharmaceutical Chemistry, Department of Biochemistry, Chemistry and Pharmacy, Goethe University Frankfurt, Max-von-Laue-Straße 9, 60438 Frankfurt, Germany

4. Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Straße 15, 60438 Frankfurt, Germany

Abstract

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.

Funder

Structural Genomics Consortium

EUbOPEN

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

Link

https://www.mdpi.com/1420-3049/28/23/7912/pdf

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