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

Abstract

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.