RESUMO
In the title compound, C(23)H(17)Cl(2)F(3)N(2)O(3), the mol-ecular conformation is significantly strained: atoms O, C(=O) and C attached to the central benzene ring deviate from its plane by 0.118â (2), 0.139â (2) and 0.174â (2)â Å, respectively. In the crystal, weak C-Hâ¯O inter-actions link the mol-ecules into chains along [110]. The crystal packing exhibits short inter-molecular Clâ¯F [2.9840â (16)â Å] and Clâ¯Cl [3.2957â (12)â Å] contacts.
RESUMO
To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition growth rate of human lung cancer cell (A549) and human endometrial adenocarcinoma cell (Ishikawa) in vitro was evaluated. The preliminary assay results showed that compounds 6j, 7o and 8c exhibited good anti-tumor activities and excellent selectivity for the Ishikawa cell, may be potential anti-tumor agents.
Assuntos
Amidas/química , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Química Farmacêutica/métodos , Diflunisal/análogos & derivados , Diflunisal/síntese química , Neoplasias/tratamento farmacológico , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Linhagem Celular Tumoral , Cristalografia por Raios X/métodos , Diflunisal/farmacologia , Desenho de Fármacos , Humanos , Concentração Inibidora 50 , Modelos Químicos , Estrutura MolecularRESUMO
To improve the medicinal activity, the structure of diflunisal has been modified. Twenty-one amide derivatives of diflunisal were synthesized starting from diflunisal in three steps with total yields from 72% to 89%. All compounds were identified by (1)H NMR, MS, and elemental analysis. The anti-inflammatory and analgesic activities for 19 compounds were evaluated. It was found that 5m possesses an excellent anti-inflammatory activity and a good analgesic activity, maybe a potential anti-inflammatory agent.