Abstract
The synthesis and antitumor activity in normoxic and hypoxic conditions of a series of pyrazolo[5,1-c][1,2,4]benzotriazine and its related analogues are reported. All compounds were tested on human colorectal adenocarcinoma cell line HCT-8 and for compounds 15 and 20, which show to have selective cytotoxicity in hypoxic and in normoxic conditions respectively, ROS production, cell cycle, and DNA fragmentation were measured. This preliminary study encouraged us to consider 15 and 20 as interesting leads for further optimization.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Cycle / drug effects
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Cell Hypoxia / drug effects*
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Cell Proliferation / drug effects*
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Drug Screening Assays, Antitumor
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Humans
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Oxygen / pharmacology*
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology
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Reactive Oxygen Species / metabolism
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Triazines / chemical synthesis*
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Triazines / chemistry
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Triazines / pharmacology
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Tumor Cells, Cultured / drug effects
Substances
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Antineoplastic Agents
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Pyrazoles
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Reactive Oxygen Species
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Triazines
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Oxygen