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Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)‑<i>s</i>‑triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades
Published 2022“…The antiproliferative activity of the novel <i>mono</i>- and <i>bis</i>(dimethylpyrazolyl)-<i>s</i>-triazine derivatives was studied against three cancer cell lines, namely, MCF-7, HCT-116, and HepG2. <i>N</i>-(4-Bromophenyl)-4-(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine <b>4f</b>, <i>N</i>-(4-chlorophenyl)-4,6-bis(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-1,3,5-triazin-2-amine <b>5c</b>, and 4,6-<i>bis</i>(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-<i>N</i>-(4-methoxyphenyl)-1,3,5-triazin-2-amine <b>5d</b> showed promising activity against these cancer cells: <b>4f</b> [(IC<sub>50</sub> = 4.53 ± 0.30 μM (MCF-7); 0.50 ± 0.080 μM (HCT-116); and 3.01 ± 0.49 μM (HepG2)]; <b>5d</b> [(IC<sub>50</sub> = 3.66 ± 0.96 μM (HCT-116); and 5.42 ± 0.82 μM (HepG2)]; and <b>5c</b> [(IC<sub>50</sub> = 2.29 ± 0.92 μM (MCF-7)]. …”
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Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)‑<i>s</i>‑triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades
Published 2022“…The antiproliferative activity of the novel <i>mono</i>- and <i>bis</i>(dimethylpyrazolyl)-<i>s</i>-triazine derivatives was studied against three cancer cell lines, namely, MCF-7, HCT-116, and HepG2. <i>N</i>-(4-Bromophenyl)-4-(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine <b>4f</b>, <i>N</i>-(4-chlorophenyl)-4,6-bis(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-1,3,5-triazin-2-amine <b>5c</b>, and 4,6-<i>bis</i>(3,5-dimethyl-1<i>H</i>-pyrazol-1-yl)-<i>N</i>-(4-methoxyphenyl)-1,3,5-triazin-2-amine <b>5d</b> showed promising activity against these cancer cells: <b>4f</b> [(IC<sub>50</sub> = 4.53 ± 0.30 μM (MCF-7); 0.50 ± 0.080 μM (HCT-116); and 3.01 ± 0.49 μM (HepG2)]; <b>5d</b> [(IC<sub>50</sub> = 3.66 ± 0.96 μM (HCT-116); and 5.42 ± 0.82 μM (HepG2)]; and <b>5c</b> [(IC<sub>50</sub> = 2.29 ± 0.92 μM (MCF-7)]. …”
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