4.6 Article

Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells

Journal

NEW JOURNAL OF CHEMISTRY
Volume 42, Issue 16, Pages 13784-13789

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8nj02388c

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Funding

  1. CSIC Grupos [654, 983]
  2. PEDECIBA Quimica
  3. Spanish MINECO
  4. European Regional Development Fund (ERDF) [CTQ2014-56362-C2-1-P]
  5. ANII (Agencia Nacional de Investigacion e Innovacion)

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Inspired by diverse marine bioactive compounds, the principle of molecular hybridization was applied to produce a series of new compounds combining diverse heterocyclic systems (oxa/thiazoles and tetrahydropyrans) via a triazole ring, attempting to increase the activity of individual building blocks. These new compounds exhibit a highly interesting antiproliferative activity against different human tumour cells and good selectivity when compared to normal cells. The formation of reactive oxygen species and the interaction with P-gp were also evaluated for the lead compounds.

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