Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives

Mozna H. Khraiwesh; Clarence M. Lee; Yakini Brandy; Emmanuel S. Akinboye; Solomon Berhe; Genelle Gittens; Muneer M. Abbas; Franklin R. Ampy; Mohammad Ashraf; Oladapo Bakare

doi:10.1007/s12272-012-0103-1

Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives

Mozna H. Khraiwesh, Clarence M. Lee, Yakini Brandy, Emmanuel S. Akinboye, Solomon Berhe, Genelle Gittens, Muneer M. Abbas, Franklin R. Ampy, Mohammad Ashraf, Oladapo Bakare

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

15 Scopus citations

Abstract

The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC ₅₀ = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from 0.7 μM to 6.1 μM (p < 0.05). Studies of the cytotoxic activities of these compounds on a Balb/C 3T3 mouse fibroblast cell line revealed that four of these compounds, IMDNQ1, IMDNQ2, IMDNQ3, and IMDNQ10 displayed selectivity indices of 60.25, 53.97, 31.83, and 275.3, respectively, rendering them significantly (p < 0.05) more selective in inhibiting the parasite growth than nifurtimox (selectivity index = 10.86).

Original language	English (US)
Pages (from-to)	27-33
Number of pages	7
Journal	Archives of Pharmacal Research
Volume	35
Issue number	1
DOIs	https://doi.org/10.1007/s12272-012-0103-1
State	Published - Jan 2012
Externally published	Yes

Keywords

Chagas disease
Cytotoxicity
Epimastigotes
Fibroblasts
Imido-substituted 1,4-naphthoquinone
Trypanosoma cruzi

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery
Organic Chemistry

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10.1007/s12272-012-0103-1

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title = "Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives",

abstract = "The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC 50 = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from 0.7 μM to 6.1 μM (p < 0.05). Studies of the cytotoxic activities of these compounds on a Balb/C 3T3 mouse fibroblast cell line revealed that four of these compounds, IMDNQ1, IMDNQ2, IMDNQ3, and IMDNQ10 displayed selectivity indices of 60.25, 53.97, 31.83, and 275.3, respectively, rendering them significantly (p < 0.05) more selective in inhibiting the parasite growth than nifurtimox (selectivity index = 10.86).",

keywords = "Chagas disease, Cytotoxicity, Epimastigotes, Fibroblasts, Imido-substituted 1,4-naphthoquinone, Trypanosoma cruzi",

author = "Khraiwesh, {Mozna H.} and Lee, {Clarence M.} and Yakini Brandy and Akinboye, {Emmanuel S.} and Solomon Berhe and Genelle Gittens and Abbas, {Muneer M.} and Ampy, {Franklin R.} and Mohammad Ashraf and Oladapo Bakare",

note = "Funding Information: This work was supported in part by the WBHR-LSAMP Program, NSF#0401723 and by an NIH grant from the Research Centers in Minority Institutions (RCMI) Program of the Division of Research Infrastructure, National Center for Research Resources (RCMI-NIH 2G12RR003048).",

year = "2012",

month = jan,

doi = "10.1007/s12272-012-0103-1",

language = "English (US)",

volume = "35",

pages = "27--33",

journal = "Archives of Pharmacal Research",

issn = "0253-6269",

publisher = "Pharmaceutical Society of Korea",

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T1 - Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives

AU - Khraiwesh, Mozna H.

AU - Lee, Clarence M.

AU - Brandy, Yakini

AU - Akinboye, Emmanuel S.

AU - Berhe, Solomon

AU - Gittens, Genelle

AU - Abbas, Muneer M.

AU - Ampy, Franklin R.

AU - Ashraf, Mohammad

AU - Bakare, Oladapo

N1 - Funding Information: This work was supported in part by the WBHR-LSAMP Program, NSF#0401723 and by an NIH grant from the Research Centers in Minority Institutions (RCMI) Program of the Division of Research Infrastructure, National Center for Research Resources (RCMI-NIH 2G12RR003048).

PY - 2012/1

Y1 - 2012/1

N2 - The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC 50 = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from 0.7 μM to 6.1 μM (p < 0.05). Studies of the cytotoxic activities of these compounds on a Balb/C 3T3 mouse fibroblast cell line revealed that four of these compounds, IMDNQ1, IMDNQ2, IMDNQ3, and IMDNQ10 displayed selectivity indices of 60.25, 53.97, 31.83, and 275.3, respectively, rendering them significantly (p < 0.05) more selective in inhibiting the parasite growth than nifurtimox (selectivity index = 10.86).

AB - The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC 50 = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from 0.7 μM to 6.1 μM (p < 0.05). Studies of the cytotoxic activities of these compounds on a Balb/C 3T3 mouse fibroblast cell line revealed that four of these compounds, IMDNQ1, IMDNQ2, IMDNQ3, and IMDNQ10 displayed selectivity indices of 60.25, 53.97, 31.83, and 275.3, respectively, rendering them significantly (p < 0.05) more selective in inhibiting the parasite growth than nifurtimox (selectivity index = 10.86).

KW - Chagas disease

KW - Cytotoxicity

KW - Epimastigotes

KW - Fibroblasts

KW - Imido-substituted 1,4-naphthoquinone

KW - Trypanosoma cruzi

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Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives

Abstract

Keywords

ASJC Scopus subject areas

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