RESUMO
One pot three-component PEG-SO(3)H catalyzed reaction of 4-(Pyridin-4-yl)benzaldehyde and triethyl phosphite with various primary amines afforded α-aminophosphonates with high yields by the Kabachnik-Field's reaction. These new structurally diversified set of α-aminophosphonates (4a-j) were evaluated for their anti-tumor activity on human chronic myeloid leukemia cells (K 562), human colon carcinoma cells (Colo 205) along with non-cancerous human embryonic kidney cells (HEK 293). They showed moderate activity on both cancerous cells and non-cancerous cells.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Técnicas de Química Sintética/métodos , Organofosfonatos/síntese química , Organofosfonatos/farmacologia , Polietilenoglicóis/química , Ácidos Sulfônicos/química , Antineoplásicos/química , Catálise , Linhagem Celular Tumoral , Humanos , Organofosfonatos/químicaRESUMO
A new series of tetraphenyl bisphosphonates have been elegantly synthesized by one-pot method and were characterized by elemental analysis, FTIR, 1H, 13C, 31P NMR, mass spectra and evaluated for their in vitro antibone resorptive activity by inhibiting growth of osteoclasts. Two bisphosphonates 3g and 3f showed marked inhibition ratio (8 µM and 10 µM) and emerged as lead compounds. All compounds were tested for their antioxidant (DPPH scavenging, reducing power and inhibition of lipid peroxidation). They exhibited potent in vitro antioxidant activity dose-dependently.
