Synthesis of amidine and bis amidine derivatives and their evaluation for anti-inflammatory and anticancer activity.
Arya S, Kumar N, Roy P, Sondhi SM.
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.