Abstract
A series of bis-intercalators bearing the 1,8-naphthalimide chromophore has been synthesized and in vitro activities determined. Most compounds have higher activities in HT-29 than the leader compounds Mitonafide and Amonafide. One of them (22) was selected for in vivo studies and presents an interesting activity in MX-1 and OVCAR models. (22) also acts as antitopoisomerase II.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenine
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Humans
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Imides / chemical synthesis*
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Imides / chemistry
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Imides / pharmacology
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Intercalating Agents / chemical synthesis*
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Intercalating Agents / pharmacology
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Isoquinolines / chemical synthesis*
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Isoquinolines / chemistry
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Isoquinolines / pharmacology
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Mice
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Naphthalenes / chemical synthesis*
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Naphthalenes / chemistry
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Naphthalenes / pharmacology
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Naphthalimides
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Neoplasms, Experimental / drug therapy
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Organophosphonates
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Structure-Activity Relationship
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Tumor Cells, Cultured / drug effects
Substances
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Antineoplastic Agents
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Imides
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Intercalating Agents
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Isoquinolines
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Naphthalenes
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Naphthalimides
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Organophosphonates
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mitonafide
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amonafide
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Adenine