2-Amino-4-aryl-5-oxo-4,5-dihydropyrano[3,2-c]chromene-3-carbonitriles with Microtubule-Disruptive, Centrosome-Declustering, and Antiangiogenic Effects in vitro and in vivo.


Journal

ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013

Informations de publication

Date de publication:
18 05 2022
Historique:
revised: 25 02 2022
received: 02 02 2022
pubmed: 1 3 2022
medline: 21 5 2022
entrez: 28 2 2022
Statut: ppublish

Résumé

A series of fifteen 2-amino-4-aryl-5-oxo-4,5-dihydropyrano[3,2-c]chromene-3-carbonitriles (1 a-o) were synthesized via a three-component reaction of 4-hydroxycoumarin, malononitrile, and diversely substituted benzaldehydes or pyridine carbaldehydes. The compounds were tested for anticancer activities against a panel of eight human tumor cell lines. A few derivatives with high antiproliferative activities and different cancer cell specificity were identified and investigated for their modes of action. They led to microtubule disruption, centrosome de-clustering and G2/M cell cycle arrest in 518 A2 melanoma cells. They also showed anti-angiogenic effects in vitro and in vivo.

Identifiants

pubmed: 35226402
doi: 10.1002/cmdc.202200064
pmc: PMC9311119
doi:

Substances chimiques

Angiogenesis Inhibitors 0
Benzopyrans 0
N-methylacetamide-oxotremorine M 3854-07-7
Oxotremorine 5RY0UWH1JL

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e202200064

Informations de copyright

© 2022 The Authors. ChemMedChem published by Wiley-VCH GmbH.

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Auteurs

Leonhard H F Köhler (LHF)

Organic Chemistry Laboratory, University of Bayreuth, Universitätsstraße 30, 95447, Bayreuth, Germany.

Sebastian Reich (S)

Organic Chemistry Laboratory, University of Bayreuth, Universitätsstraße 30, 95447, Bayreuth, Germany.

Gerrit Begemann (G)

Department of Biology, University of Bayreuth, Universitätsstraße 30, 95447, Bayreuth, Germany.

Rainer Schobert (R)

Organic Chemistry Laboratory, University of Bayreuth, Universitätsstraße 30, 95447, Bayreuth, Germany.

Bernhard Biersack (B)

Organic Chemistry Laboratory, University of Bayreuth, Universitätsstraße 30, 95447, Bayreuth, Germany.

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Classifications MeSH