Serendipitous Identification of Azine Anticancer Agents by a Privileged Scaffold Morphing Strategy

Silvia Cesarini; Ilaria Vicenti; Federica Poggialini; Silvia Filippi; Eleonora Mancin; Lia Fiaschi; Elisa De Marchi; Federica Giammarino; Chiara Vagaggini; Bruno Mattia Bizzarri; Raffaele Saladino; Elena Dreassi; Maurizio Zazzi; Lorenzo Botta

doi:10.20944/preprints202402.0994.v1

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preprints.org > chemistry and materials science > medicinal chemistry > doi: 10.20944/preprints202402.0994.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Serendipitous Identification of Azine Anticancer Agents by a Privileged Scaffold Morphing Strategy

Bruno Mattia Bizzarri

Version 1 : Received: 16 February 2024 / Approved: 19 February 2024 / Online: 19 February 2024 (16:08:29 CET)

A peer-reviewed article of this Preprint also exists.

Cesarini, S.; Vicenti, I.; Poggialini, F.; Filippi, S.; Mancin, E.; Fiaschi, L.; De Marchi, E.; Giammarino, F.; Vagaggini, C.; Bizzarri, B.M.; Saladino, R.; Dreassi, E.; Zazzi, M.; Botta, L. Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy. Molecules 2024, 29, 1452. Cesarini, S.; Vicenti, I.; Poggialini, F.; Filippi, S.; Mancin, E.; Fiaschi, L.; De Marchi, E.; Giammarino, F.; Vagaggini, C.; Bizzarri, B.M.; Saladino, R.; Dreassi, E.; Zazzi, M.; Botta, L. Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy. Molecules 2024, 29, 1452.

Abstract

The use of privileged scaffolds as starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that allow to modify the privileged framework chosen and better explore the chemical space around it. In this study, two series of highly functionalized pyrimidine and pyridine derivatives were synthesized by scaffold morphing approach of triazine compounds obtained previously as antiviral agents. Newly synthesized azines were evaluated against lymphoma, hepatocarcinoma, and colon epithelial carcinoma cells showing in five cases acceptable to good anticancer activity associated to low cytotoxicity on healthy fibroblasts. Finally, ADME in vitro studies were conducted on the best derivatives of the two series showing good passive permeability and resistance to metabolic degradation.

Keywords

Privileged scaffold; triazines; pyrimidines; pyridines; scaffold morphing; anticancer activity.

Subject

Chemistry and Materials Science, Medicinal Chemistry

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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