1428745-89-4Relevant academic research and scientific papers
Mannich Curcuminoids as Potent Anticancer Agents
Gyuris, Márió,Hackler, László,Nagy, Lajos I.,Alf?ldi, Róbert,Rédei, Eszter,Marton, Annamária,Vellai, Tibor,Faragó, Nóra,ózsvári, Béla,Hetényi, Anasztázia,Tóth, Gábor K.,Sipos, Péter,Kanizsai, Iván,Puskás, László G.
, (2017/07/11)
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.
NOVEL MEDICINAL COMPOUNDS
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Page/Page column 48-49, (2013/04/10)
The invention relates to novel compounds of general formula (I), and their preparation, pharmaceutical preparations containing compounds of general formula (I), and the use of these compounds in therapeutic procedures. The invention also relates to compounds of general formula (VI), which can be used as intermediates in the processes for the preparation of compounds of general formula (I).
