Abstract |
A selection of new chromeno[2,3-b] pyridines was prepared from chromenylacrylonitriles and N-substituted piperazines, using a novel and efficient synthetic procedure. The compounds were tested for their anticancer activity using breast cancer cell lines MCF-7, Hs578t and MDA-MB-231 and the non-neoplastic cell line MCF-10A for toxicity evaluation. In general, compounds showed higher activity towards the luminal breast cancer subtype (MCF-7), competitive with the reference compound Doxorubicin. The in vivo toxicity assay using C. elegans demonstrated a safe profile for the most active compounds. Chromene 3f revealed a promising drug profile, inhibiting cell growth and proliferation, inducing cell cycle arrest in G2/M phase, apoptosis and microtubule destabilization. The new compounds presented exciting bioactive features and may be used as lead compounds in cancer related drug discovery.
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Authors | Sofia Oliveira-Pinto, Olívia Pontes, Diogo Lopes, Belém Sampaio-Marques, Marta D Costa, Luísa Carvalho, Céline S Gonçalves, Bruno M Costa, Patrícia Maciel, Paula Ludovico, Fátima Baltazar, Fernanda Proença, Marta Costa |
Journal | Bioorganic chemistry
(Bioorg Chem)
Vol. 100
Pg. 103942
(07 2020)
ISSN: 1090-2120 [Electronic] United States |
PMID | 32450388
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2020 Elsevier Inc. All rights reserved. |
Chemical References |
- Antineoplastic Agents
- Benzopyrans
- Pyrimidines
- chromeno(2,3-b)-pyrimidine
- Doxorubicin
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Topics |
- Animals
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology)
- Apoptosis
(drug effects)
- Benzopyrans
(chemical synthesis, chemistry, pharmacology)
- Breast Neoplasms
(metabolism, pathology)
- Caenorhabditis elegans
(drug effects, physiology)
- Cell Line, Tumor
- Cell Proliferation
(drug effects)
- Doxorubicin
(pharmacology)
- Drug Screening Assays, Antitumor
- Female
- G2 Phase Cell Cycle Checkpoints
(drug effects)
- Humans
- M Phase Cell Cycle Checkpoints
(drug effects)
- Pyrimidines
(chemical synthesis, chemistry, pharmacology)
- Structure-Activity Relationship
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