Design, synthesis and pharmacological evaluation of novel substituted quinoline-2-carboxamide derivatives as human dihydroorotate dehydrogenase (hDHODH) inhibitors and anticancer agents

• Substituted quinoline-2-carboxamide derivatives were designed and synthesized as hDHODH inhibitors.
• Synthesized compounds were characterized by 1H and 13C NMR, IR, MS and elemental analysis.
• Human DHODH enzyme inhibition assay was used to screen the compounds.
• Compounds were also evaluated for antiproliferative effects against the cancer cell lines.
• Compounds showed good potential to be hDHODH inhibitors.

In continuation of our research for novel human dihydroorotate dehydrogenase (hDHODH) inhibitors, herein we reported design, synthesis and pharmacological evaluation of novel substituted quinoline-2-carboxamide derivatives. Human DHODH enzyme inhibition assay was used to screen the synthesized compounds as hDHODH inhibitors. The synthesized compounds were also evaluated for their antiproliferative effects on the cancer cell lines (HEP-3B and A-375) to establish a proof as anticancer agents. The chemical structures of compounds were confirmed by 1H, 13C NMR, IR, MS and elemental analysis. The purity of compounds was also checked by HPLC analysis. Compounds with bulky groups (–OCH3, –OCF3 and –CF3) at C6-position of quinoline ring showed good activity.

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