Mannich Curcuminoids as Potent Anticancer Agents

Márió Gyuris, László Hackler, Lajos I. Nagy, Róbert Alföldi, Eszter Rédei, Annamária Marton, T. Vellai, Nóra Faragó, Béla Ózsvári, A. Hetényi, G. Tóth, Péter Sipos, Iván Kanizsai, L. Puskás

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Abstract

A series of novel curcuminoids were synthesised for the first time via a Mannich-3CR/organocatalysed Claisen–Schmidt condensation sequence. Structure–activity relationship (SAR) studies were performed by applying viability assays and holographic microscopic imaging to these curcumin analogues for anti-proliferative activity against A549 and H1975 lung adenocarcinoma cells. The TNFα-induced NF-κB inhibition and autophagy induction effects correlated strongly with the cytotoxic potential of the analogues. Significant inhibition of tumour growth was observed when the most potent analogue 44 was added in liposomes at one-sixth of the maximally tolerated dose in the A549 xenograft model. The novel spectrum of activity of these Mannich curcuminoids warrants further preclinical investigations.

Original languageEnglish
Article numbere1700005
JournalArchiv der Pharmazie
Volume350
Issue number7
DOIs
Publication statusPublished - Jul 1 2017

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Keywords

  • Anticancer
  • Autophagy
  • Curcuminoids
  • Mannich
  • NF-κB inhibition

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

Cite this

Gyuris, M., Hackler, L., Nagy, L. I., Alföldi, R., Rédei, E., Marton, A., Vellai, T., Faragó, N., Ózsvári, B., Hetényi, A., Tóth, G., Sipos, P., Kanizsai, I., & Puskás, L. (2017). Mannich Curcuminoids as Potent Anticancer Agents. Archiv der Pharmazie, 350(7), [e1700005]. https://doi.org/10.1002/ardp.201700005