Synthesis of amidine and bis amidine derivatives and their evaluation for anti-inflammatory and anticancer activity

2-Cyanopyridine (1a), 4-cyanopyridine (1b), 2-cyanopyrazine (1c) on condensation with mono amines (2a–c) and diamines (4a–c) in the presence of sodium methoxide as catalyst gave amidine derivatives (3a–i) and bis amidine derivatives (5a–i) in good yields. All these compounds were fully characterized by spectroscopic means and elemental analysis. On screening for anti-inflammatory activity and for in vitro anticancer activity compounds 5c and 5d exhibited good anti-inflammatory activity whereas compounds 5d breast (T47D), 5h, 5i lung (NCI H-522), 5i colon (HCT-15), 3c, 3h, 5i ovary (PA-1) and 3c, 5b, 5h liver (HepG2) exhibited good anticancer activity.

Several amidine (3a–i) and bis amidine (5a–i) derivatives have been synthesized. Some of the compounds exhibited good anti-inflammatory and anticancer activity.Figure optionsDownload as PowerPoint slideHighlights
► Several amidine and bis amidine derivatives have been synthesized.
► A few compounds show good anti-inflammatory activity.
► Some of the compounds exhibited good anticancer activity.