14 research outputs found
Synthesis and antiproliferative activities of quebecol and its analogs
Simple and efficient synthesis of quebecol and a number of its analogs was accomplished in five steps. The synthesized compounds were evaluated for antiproliferative activities against human cervix adenocarcinoma (HeLa), human ovarian carcinoma (SK-OV-3), human colon carcinoma (HT-29), and human breast adenocarcinoma (MCF-7) cancer cell lines. Among all the compounds, 7c, 7d, 7f, and 8f exhibited antiproliferative activities against four tested cell lines with inhibition over 80% at 75 ÎĽM after 72 h, whereas, compound 7b and 7g were more selective towards MCF-7 cell line. The IC50 values for compounds 7c, 7d, and 7f were 85.1 ÎĽM, 78.7 ÎĽM, and 80.6 ÎĽM against MCF-7 cell line, respectively, showing slightly higher antiproliferative activtiy than the synthesized and isolated quebecol with an IC50 value of 104.2 ÎĽM against MCF-7.
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Synthesis of Aza-Fused Isoquinolines through Domino Cross-Aldol Condensation and Palladium-Catalyzed Intramolecular Direct Arylation
A straightforward method has been
developed for the synthesis of
aroyl-substituted imidazo-/benzimidazo-fused isoquinolines. The cascade
reaction proceeds via a cross-aldol condensation of 2-(1<i>H</i>-imidazol-1-yl/benzimidazolyl-1-yl)-1-arylethanones and 2-bromobenzaldehyde
followed by palladium-catalyzed intramolecular C–H functionalization.
This approach offers a simple and efficient alternative one-pot protocol
for the assembly of imidazo/benzimidazoÂ[2,1-<i>a</i>]Âisoquinolines
in moderate to good yields