Abstract
Three series of monoquinolines consisting of a 1,4-bis(3-aminopropyl)piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ, and one of them cured mice infected by Plasmodium berghei.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / chemistry
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Antimalarials / pharmacology
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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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Chloroquine / pharmacology
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Drug Resistance
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Female
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Humans
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Malaria / drug therapy
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Mice
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology
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Plasmodium berghei
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Plasmodium falciparum / drug effects
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Antimalarials
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Antineoplastic Agents
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Piperazines
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Quinolines
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Chloroquine