| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1393076 | European Journal of Medicinal Chemistry | 2011 | 9 Pages |
A series of novel 2-amino-3-cyano-6-(1H-indol-3-yl)-4-phenylpyridine derivatives were synthesized and their cytotoxic activity against A549, H460, HT-29 and SMMC-7721 cell lines was evaluated in vitro. Among them, ten compounds (10, 11, 14, 16, 17, 26, 27, 29, 30 and 31) displayed excellent anti-tumor activity against different cell lines. The most promising compound 27 showed strong anti-tumor activity against A549, H460, HT-29 and SMMC-7721 cell lines with IC50 values of 22, 0.23, 0.65 and 0.77 nM, which were 2.6-, 83-, 1.1 × 103- and 2.0 × 103- fold more active than MX-58151 (IC50 values of 0.058, 0.019, 0.70 and 1.53 μM), respectively.
Graphical abstractA series of novel 2-amino-3-cyano-6-(1H-indol-3-yl)-4-phenylpyridine derivatives were synthesized and their cytotoxic activity against A549, H460, HT-29 and SMMC-7721 cell lines was evaluated in vitro by the standard MTT assay.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Introduction of indole core improved the cytotoxicity of 4,6-diaryl-2-amino-3-cyanopyridines. ► Ten compounds showed potent cytotoxicity against different cell lines with IC50 values in nM range. ► Some compounds exhibited excellent selectivity against H460 or HT-29 cell lines. ► Compound 27 showed the strongest cytotoxicity against four cell lines with IC50 values in nM range.
