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Mannich Curcuminoids as Potent Anticancer Agents
Author(s) -
Gyuris Márió,
Hackler László,
Nagy Lajos I.,
Alföldi Róbert,
Rédei Eszter,
Marton Annamária,
Vellai Tibor,
Faragó Nóra,
Ózsvári Béla,
Hetényi Anasztázia,
Tóth Gábor K.,
Sipos Péter,
Kanizsai Iván,
Puskás László G.
Publication year - 2017
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700005
Subject(s) - chemistry , curcumin , a549 cell , liposome , pharmacology , stereochemistry , cytotoxicity , structure–activity relationship , combinatorial chemistry , biochemistry , in vitro , biology
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.