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Research Article

Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles

, , , , , , & show all
Pages 778-785 | Received 04 Jul 2014, Accepted 29 Sep 2014, Published online: 27 Aug 2015

Figures & data

Figure 1. Synthetic route of newly synthesized componds 4a–h.

Figure 1. Synthetic route of newly synthesized componds 4a–h.

Table 1. The anticancer screening data of etodolac triazoles, 4b and 4f.

Table 2. Anti-HCV NS5B RdRp activity of etodolac derivatives.

Figure 2. Glide-XP predicted binding model of compound (S)-4a within the TP-II of HCV NS5B polymerse. Amino acid residues are shown as stick model with the atoms colored as carbon – green, hydrogen – white, nitrogen – blue oxygen – red and sulfur – yellow whereas inhibitor is shown as ball and stick model with the same color scheme as above except carbon atoms are represented in orange. Water molecules are shown as stick model. Dotted black line indicates hydrogen bonding interaction whereas dotted pink line indicates potential electrostatic contact with distances in Å (please view this figure in color mode in the online version).

Figure 2. Glide-XP predicted binding model of compound (S)-4a within the TP-II of HCV NS5B polymerse. Amino acid residues are shown as stick model with the atoms colored as carbon – green, hydrogen – white, nitrogen – blue oxygen – red and sulfur – yellow whereas inhibitor is shown as ball and stick model with the same color scheme as above except carbon atoms are represented in orange. Water molecules are shown as stick model. Dotted black line indicates hydrogen bonding interaction whereas dotted pink line indicates potential electrostatic contact with distances in Å (please view this figure in color mode in the online version).

Figure 3. Percent growth inhibition graphs of compound 4a, SGK-238 on liver cancer cell lines (Huh7, Mahlavu, HepG2, FOCUS).

Figure 3. Percent growth inhibition graphs of compound 4a, SGK-238 on liver cancer cell lines (Huh7, Mahlavu, HepG2, FOCUS).

Table 3. IC50 values in µM concentrations for compound 4a with 72 h of treatment on liver cancer cell linesa.

Supplemental material

Supplemental Material.pdf

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