Abstract
A new class of pyridobenzophenoxazine compounds has been developed as topoisomerase II inhibitors for anticancer chemotherapy. These compounds were designed based on a proposed model of a quinobenzoxazine self-assembly complex on DNA. They showed excellent inhibitory effects on several tumor cell lines with nanomolar IC50 values. Their cytotoxic potency correlates with their ability to unwind DNA and inhibit topoisomerase II.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
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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DNA, Superhelical / drug effects
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Drug Design*
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Oxazines / chemical synthesis*
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Oxazines / chemistry
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Oxazines / pharmacology
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Structure-Activity Relationship
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Topoisomerase II Inhibitors*
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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DNA, Superhelical
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Enzyme Inhibitors
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Oxazines
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Topoisomerase II Inhibitors