Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-Tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones
AQUEOUS SOLUTION;
ARTICLE;
CHEMICAL STRUCTURE;
DRUG DESIGN;
DRUG FORMULATION;
DRUG POTENCY;
DRUG SYNTHESIS;
EVALUATION;
HEART MUSCLE ISCHEMIA;
HUMAN;
IN VITRO STUDY;
PHYSICAL CHEMISTRY;
SOLUBILITY;
STROKE;
STRUCTURE ACTIVITY RELATION;
SYNTHESIS;
3H]nicotinamide adenine dinucleotide (67 mCi/mmol), 75 μg/mL PARP enzyme, and various concentrations of the compounds to be tested. The reaction is initiated by incubating the mixture at 25°C. After 15 min of incubation, the reaction was terminated by adding 500 mL of ice cold 20% (w/v) trichloroacetic acid. The precipitate formed is transferred onto a glass fiber filter (Packard Unifilter-GF/B) and washed three times with ethanol. After the filter is dried, the radioactivity is determined by scintillation counting.
3H]nicotinamide adenine dinucleotide (67 mCi/mmol), 75 μg/mL PARP enzyme, and various concentrations of the compounds to be tested. The reaction is initiated by incubating the mixture at 25°C. After 15 min of incubation, the reaction was terminated by adding 500 mL of ice cold 20% (w/v) trichloroacetic acid. The precipitate formed is transferred onto a glass fiber filter (Packard Unifilter-GF/B) and washed three times with ethanol. After the filter is dried, the radioactivity is determined by scintillation counting.
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Lopes R.S.C., Lopes C.L., Heathcock C.H. Tetrahedron Lett. 33:1992;6775.
