1242543-31-2

Upstream product

• 41661-47-6 piperidin-4-one 
• 455-19-6 4-Trifluoromethylbenzaldehyde 
• 41979-39-9 4-piperidone hydrochloride 

Downstream Products

• 1636872-76-8 2-oxo-2-((3E,5E)-4-oxo-3,5-bis(4-(trifluoromethyl)benzylidene)piperidin-1-yl)ethyl morpholine-4-carbodithioate 
• 1636872-33-7 C₂₃H₁₆ClF₆NO₂ 

Relevant academic research and scientific papers

p-Trifluoromethyl- and p-pentafluorothio-substituted curcuminoids of the 2,6-di[(E)-benzylidene)]cycloalkanone type: Syntheses and activities against Leishmania major and Toxoplasma gondii parasites

A series of the title curcuminoids with structural variance in the heteroatom of the cycloalkanone and the p-substituents of the phenyl rings were tested for their activities against Leishmania major and Toxoplasma gondii parasites. The majority of them showed high activities against both parasite forms with EC50 values in the sub-micromolar concentration range. Bis(p-pentafluorothio)-substituted 3,5-di[(E)-benzylidene]piperidin-4-one 1b was not just noticeable antiparasitic, but also exhibited a considerable selectivity for L. major promastigotes over normal Vero cells. While derivatives differing only in the p-phenyl substituents being CF3 or SF5 showed similar antiparasitic activities, the cyclic ketone hub was more decisive both for the anti-parasitic activities and the selectivities for the parasites vs. normal cells. QSAR calculations confirmed the observed structure–activity relations and suggested structural variations for a further improvement of the antiparasitic activity. Docking studies based on DFT calculations revealed L. major pteridine reductase 1 as a likely molecular target protein of the title compounds.

Disubstituted aryl compound and application thereof

The invention relates to bis-substituted aryl compounds and application thereof. The structure of the bis-substituted aryl compounds is disclosed as Formula I, II or III. The experimental verification detects that the bis-substituted aryl compounds can be

C5-curcuminoid-dithiocarbamate based molecular hybrids: Synthesis and anti-inflammatory and anti-cancer activity evaluation

A series of C5-curcumin bearing morpholine based dithiocarbamates was synthesized. Molinspiration and Osiris software were used for theoretical prediction of physico-chemical properties of these molecules and the majority of the hybrids showed theoretical physico-chemical properties similar or better than curcumin. These hybrids (4a-4v) were evaluated for in vitro cytotoxicity on chronic myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines, and down modulation of TNF-α-induced NF-κB activation at 5 μM. Most of the hybrids exhibit higher cytotoxicity against KBM5 cells compared to HCT116 cell lines. Further, all the hybrids showed potential to suppress the TNF-α-induced NF-κB activation at 5 μM KBM5 cells and seventeen hybrids have shown higher potential to inhibit NF-κB activation in comparison to curcumin.

COMPOSITIONS AND METHODS FOR INHIBITION OF CANCERS

Methods and compositions for treating cancers, including ovarian cancers, are described. The compositions generally include a redox based curcumin derivative, diarylidenylpiperiden-4-one (DAP) having a hydroxylamine moiety attached thereto.