Mannich Curcuminoids as Potent Anticancer Agents

Gyuris, Márió and Hackler, László and Nagy, Lajos and Alföldi, Róbert and Rédei, Eszter and Marton, Annamária and Vellai, Tibor and Faragó, Nóra and Hetényi, Anasztázia and Puskás, László (2017) Mannich Curcuminoids as Potent Anticancer Agents. ARCHIV DER PHARMAZIE, 350 (7). pp. 1-22. ISSN 0365-6233

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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.

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