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Mannich Curcuminoids as Potent Anticancer Agents

Archiv der Pharmazie, 2017 | M. Gyuris, L. Hackler, L. Nagy, R. Alföldi, E. Rédei, A. Marton, T. Vellai, N. Faragó, B. Ózsvári, A. Hetényi, G. Tóth, P. Sipos, I. Kanizsai and L. Puskás

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.

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