1.
Bioorg Med Chem Lett
; 30(4): 126910, 2020 02 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-31882300
RESUMO
Six N-nitroaryl-2-amino-1,3-dichloropropane derivatives have been prepared and evaluated against 18 cancer cell lines and two non-cancerous cell lines. Analysis of cell viability data and IC50 values indicated that the presence of a trifluoromethyl group in the nitroaryl moiety is an important structural feature associated with the compounds' cytotoxicities.
Assuntos
Antineoplásicos/síntese química , Propano/análogos & derivados , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Metilação , Pró-Fármacos/síntese química , Pró-Fármacos/química , Pró-Fármacos/farmacologia , Propano/síntese química , Propano/química , Propano/farmacologia , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 26(24): 5851-5854, 2016 12 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27876476
RESUMO
A series of N-nitroarylated-3-chloromethyl-1,2,3,4-tetrahydroisoquinoline derivatives, several of which also possessed a trifluoromethyl substituent, were prepared and assessed as potential nitroaromatic prodrugs. The enzymatic reduction of these compounds and their cytotoxicities were studied. The compounds were cytotoxic, but this is probably not related to their enzymatic reduction.