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Unravelling the anticancer potential of functionalized chromeno[2,3-b]pyridines for breast cancer treatment.

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.
AuthorsSofia 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
JournalBioorganic chemistry (Bioorg Chem) Vol. 100 Pg. 103942 (07 2020) ISSN: 1090-2120 [Electronic] United States
PMID32450388 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2020 Elsevier Inc. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Benzopyrans
  • Pyrimidines
  • chromeno(2,3-b)-pyrimidine
  • Doxorubicin
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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