Abstract
The exceptional TOP1-targeting activity and antitumor activity of ARC-111, 1, prompted studies on similarly substituted benzo[i]phenanthridine-12-carboxylic ester and amide derivatives. These studies were extended to include 6-substituted 8,9-dimethoxy-2,3-methylenedioxy-dibenzo[c,h][2,6]naphthyridin-5-ones, which represent reversed lactam analogues of 1. Several of these analogues retained the potent TOP1-targeting activity and cytotoxicity observed for ARC-111.
Publication types
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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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Carboxylic Acids / chemical synthesis
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Carboxylic Acids / chemistry
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Carboxylic Acids / pharmacology*
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Cell Line, Tumor
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Cell Survival / drug effects
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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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Naphthyridines / chemical synthesis
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Naphthyridines / chemistry
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Naphthyridines / pharmacology*
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Phenanthridines / chemical synthesis
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Phenanthridines / chemistry
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Phenanthridines / pharmacology*
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Structure-Activity Relationship
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Topoisomerase I Inhibitors*
Substances
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Antineoplastic Agents
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Carboxylic Acids
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Enzyme Inhibitors
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Naphthyridines
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Phenanthridines
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Topoisomerase I Inhibitors
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dimethoxybenzo(i)phenanthridine-12-carboxylic acid
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topovale