RESUMO
A series of valproic acid salicylanilide esters were designed and synthesized based on the principle of prodrug. The structures of the target compounds were confirmed by MS, 1H NMR and 13C NMR. Anti-tumor activities of these compounds against K562, A549, A431 cells in vitro were investigated by MTT assay and SRB assay. The results indicated that the compounds 6h-6j were found to have stronger cell growth inhibitory action than gefitinib, and comparable to niclosamide, which are worth to be intensively studied further.
Assuntos
Antineoplásicos/síntese química , Proliferação de Células/efeitos dos fármacos , Desenho de Fármacos , Pró-Fármacos/síntese química , Salicilanilidas/síntese química , Ácido Valproico/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Ésteres , Humanos , Concentração Inibidora 50 , Células K562 , Estrutura Molecular , Pró-Fármacos/química , Pró-Fármacos/farmacologia , Salicilanilidas/química , Salicilanilidas/farmacologia , Relação Estrutura-Atividade , Ácido Valproico/química , Ácido Valproico/farmacologiaRESUMO
New sesquiterpene glycoside, cyclodipeptide and piperidine derivative were isolated from Streptomyces sp. YIM 63342. On the basis of spectral data, their structures were determined as 3R, 5R, 6S, 7E, 9R-megastigman-7-en-3,5,6,9-tetrol-9-O-ß-D-apiofuranosyl-(1â 2)-ß-D-glucopyranoside (1), cyclo (L-Pro-L-OMet) (2) and (R)-(E, E)-2-(l,3-pentadienyl) piperidine (3), together with three known compounds as N-acetyltyramine (4), lycoperodine-1 (5), cyclo(L-Pro-L-Tyr)(6).
Assuntos
Alcaloides/química , Cicloexanonas/química , Glucosídeos/química , Glicosídeos/química , Norisoprenoides/química , Streptomyces/química , Animais , Antifúngicos/química , Antifúngicos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Fusarium/efeitos dos fármacos , Humanos , Estrutura MolecularRESUMO
A novel series of prodrugs consisting of dabigatran and 2-hydroxymethyl-3,5,6-trimethylpyrazine (HTMP) were synthesized. The pharmacological results show that all of them possess the effect of anti-platelet aggregation induced by thrombin in vitro. Moreover, one of those compounds, Y-2 (ED(50) = 2.1 ± 1.3 mg/kg) shows more potent activity for inhibiting thrombosis in vivo than that of dabigatran etexilate (ED(50) = 4.4 ± 2.2 mg/kg).