RESUMO
4-Bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (3c) was first synthesized from 3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (2c) by a bromo-radical substitution reaction occurred at C-4 position by N-bromosuccinimide and 2,2'-azobisisobutyronitrile. The novel phospha sugar analogue 3c exerted high anti-proliferative effect on U937 cells evaluated by MTT in vitro methods and was much more efficient than that of Gleevec, which is known as a molecule targeting chemotherapeutical agent. The substitution of 2-phospholenes at C-3 and C-4 position with methyl groups as well as 4-bromo substituent suggests a good anti-proliferative effect.
Assuntos
Antineoplásicos/química , Óxidos P-Cíclicos/síntese química , Compostos Heterocíclicos/química , Compostos Organofosforados/síntese química , Fósforo/química , Antineoplásicos/síntese química , Antineoplásicos/toxicidade , Benzamidas , Linhagem Celular Tumoral , Óxidos P-Cíclicos/química , Óxidos P-Cíclicos/toxicidade , Compostos Heterocíclicos/síntese química , Compostos Heterocíclicos/toxicidade , Humanos , Mesilato de Imatinib , Compostos Organofosforados/química , Compostos Organofosforados/toxicidade , Piperazinas/toxicidade , Pirimidinas/toxicidadeRESUMO
A new type of dendritic molecules Gd-DTPA-XDA-D1-Glc(OH), which work as a functionalized ligand coordinating gadolinium(III) ion at the center of their frameworks with two glucose moieties on the molecular surfaces, were readily synthesized with high yield. The structures were established by IR, (1)H, (13)C NMR, and mass spectral studies. Its bio-distribution patterns were evaluated on rats.
