Hydroxy-anthraquinones as antimalarial agents

R. W. Winter; Kenneth A. Cornell; Linda L. Johnson; Loren M. Isabelle; David J. Hinrichs; Michael K. Riscoe

doi:10.1016/0960-894X(95)00326-O

Hydroxy-anthraquinones as antimalarial agents

R. W. Winter, Kenneth A. Cornell, Linda L. Johnson, Loren M. Isabelle, David J. Hinrichs, Michael K. Riscoe

Molecular Microbiology and Immunology

Research output: Contribution to journal › Article › peer-review

26 Scopus citations

Abstract

A series of hydroxy- and polyhydroxy-anthraquinones were screened for inhibitory activity against the malarial parasite, Plasmodium falciparum. Rufigallol demonstrated the most potent effects with a 50% inhibitory concentration (IC₅₀ value of ∼10.5 ng/ml (∼35 nM). Deleterious effects were exerted by rufigallol toward bone marrow progenitor cells at concentrations≥ 10 μM (3 μg/ml) where ∼30% suppression of colony growth was noted. Taking into consideration its potency and relative lack of toxicity, we believe that rufigallol should be advanced for in vivo studies. At the very least, rufigallol represents a simple, inexpensive lead drug for the development of more potent analogs.

Original language	English (US)
Pages (from-to)	1927-1932
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	5
Issue number	17
DOIs	https://doi.org/10.1016/0960-894X(95)00326-O
State	Published - Sep 7 1995

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/0960-894X(95)00326-O

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title = "Hydroxy-anthraquinones as antimalarial agents",

abstract = "A series of hydroxy- and polyhydroxy-anthraquinones were screened for inhibitory activity against the malarial parasite, Plasmodium falciparum. Rufigallol demonstrated the most potent effects with a 50% inhibitory concentration (IC50 value of ∼10.5 ng/ml (∼35 nM). Deleterious effects were exerted by rufigallol toward bone marrow progenitor cells at concentrations≥ 10 μM (3 μg/ml) where ∼30% suppression of colony growth was noted. Taking into consideration its potency and relative lack of toxicity, we believe that rufigallol should be advanced for in vivo studies. At the very least, rufigallol represents a simple, inexpensive lead drug for the development of more potent analogs.",

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T1 - Hydroxy-anthraquinones as antimalarial agents

AU - Winter, R. W.

AU - Cornell, Kenneth A.

AU - Johnson, Linda L.

AU - Isabelle, Loren M.

AU - Hinrichs, David J.

AU - Riscoe, Michael K.

PY - 1995/9/7

Y1 - 1995/9/7

N2 - A series of hydroxy- and polyhydroxy-anthraquinones were screened for inhibitory activity against the malarial parasite, Plasmodium falciparum. Rufigallol demonstrated the most potent effects with a 50% inhibitory concentration (IC50 value of ∼10.5 ng/ml (∼35 nM). Deleterious effects were exerted by rufigallol toward bone marrow progenitor cells at concentrations≥ 10 μM (3 μg/ml) where ∼30% suppression of colony growth was noted. Taking into consideration its potency and relative lack of toxicity, we believe that rufigallol should be advanced for in vivo studies. At the very least, rufigallol represents a simple, inexpensive lead drug for the development of more potent analogs.

AB - A series of hydroxy- and polyhydroxy-anthraquinones were screened for inhibitory activity against the malarial parasite, Plasmodium falciparum. Rufigallol demonstrated the most potent effects with a 50% inhibitory concentration (IC50 value of ∼10.5 ng/ml (∼35 nM). Deleterious effects were exerted by rufigallol toward bone marrow progenitor cells at concentrations≥ 10 μM (3 μg/ml) where ∼30% suppression of colony growth was noted. Taking into consideration its potency and relative lack of toxicity, we believe that rufigallol should be advanced for in vivo studies. At the very least, rufigallol represents a simple, inexpensive lead drug for the development of more potent analogs.

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Hydroxy-anthraquinones as antimalarial agents

Abstract

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