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

Affiliation
Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece;(M.K.);(D.K.);(A.D.K.)
Karelou, Maria;
ORCID
0009-0004-8554-8936
Affiliation
Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece;(M.K.);(D.K.);(A.D.K.)
Kampasis, Dionysis;
ORCID
0000-0003-2272-6622
Affiliation
Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece;(M.K.);(D.K.);(A.D.K.)
Kalampaliki, Amalia D.;
ORCID
0000-0002-7898-0868
Affiliation
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;(L.P.);(D.S.);(S.D.J.)
Persoons, Leentje;
Affiliation
Institute for Pharmaceutical Chemistry, Department of Biochemistry, Chemistry and Pharmacy, Goethe University Frankfurt, Max-von-Laue-Straße 9, 60438 Frankfurt, Germany;(A.K.);(S.K.)
Krämer, Andreas;
ORCID
0000-0003-3256-5850
Affiliation
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;(L.P.);(D.S.);(S.D.J.)
Schols, Dominique;
ORCID
0000-0001-5995-6494
Affiliation
Institute for Pharmaceutical Chemistry, Department of Biochemistry, Chemistry and Pharmacy, Goethe University Frankfurt, Max-von-Laue-Straße 9, 60438 Frankfurt, Germany;(A.K.);(S.K.)
Knapp, Stefan;
ORCID
0000-0002-3872-6558
Affiliation
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;(L.P.);(D.S.);(S.D.J.)
De Jonghe, Steven;
ORCID
0000-0002-9901-5223
Affiliation
Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece;(M.K.);(D.K.);(A.D.K.)
Kostakis, Ioannis K.

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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Editor:
Nikolaropoulos, Sotiris S.
Published in:
Molecules  
Vol. 28, No. 23 (02.12.2023)
Volume:
28
No.:
23
Date Issued:
02.12.2023
DOI:
10.3390/molecules28237912
Language:
English
Type of Resource:
Text
Keywords:
  1. quinazolines
    Typ
    Schlagwort
  1. synthesis
    Typ
    Schlagwort
  1. anti-proliferative activity
    Typ
    Schlagwort
  1. kinase inhibition
    Typ
    Schlagwort
DDC:
610 Medizin und Gesundheit

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License Holder: © 2023 by the authors.

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