Keyari, Charles M. published the artcileSynthesis of New Quinolinequinone Derivatives and Preliminary Exploration of their Cytotoxic Properties, Application of 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2013), 56(10), 3806-3819, database is CAplus and MEDLINE.
A series of 7-amino- and 7-acetamidoquinoline-5,8-diones with aryl substituents at the 2-position were synthesized, characterized, and evaluated as potential NAD(P)H:quinone oxidoreductase (NQO1)-directed antitumor agents. The synthesis of lavendamycin analogs is illustrated. Metabolism studies demonstrated that 7-amino analogs were generally better substrates for NQO1 than 7-amido analogs, as were compounds with smaller heteroaromatic substituents at the C-2 position. Surprisingly, only two compounds, 7-acetamido-2-(8′-quinolinyl)quinoline-5,8-dione and 7-amino-2-(2-pyridinyl)quinoline-5,8-dione, showed selective cytotoxicity toward the NQO1-expressing MDA468-NQ16 breast cancer cells vs. the NQO1-null MDA468-WT cells. For all other compounds, NQO1 protected against quinoline-5,8-dione cytotoxicity. Compound I showed potent activity against human breast cancer cells expressing or not expressing NQO1, with resp. IC50 values of 190 nM and 140 nM and a low NQO1-mediated reduction rate, which suggests that the mode of action of I differs from that of lavendamycin and involves an unidentified target(s).
Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Application of 1H-Pyrazole-4-boronic acid.
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https://en.wikipedia.org/wiki/Pyrazole,
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