Preparation, characterization and the anticancer activity of a novel series of triaminemonochloroplatinum(II) cations linked to anthraquinone intercalators

KF Gean; R. Ben-Shoshan; A. Ramu; I. Ringel; J. Katzhendler; D. Gibson

doi:10.1016/0223-5234(91)90193-Q

Preparation, characterization and the anticancer activity of a novel series of triaminemonochloroplatinum(II) cations linked to anthraquinone intercalators

KF Gean, R. Ben-Shoshan, A. Ramu, I. Ringel, J. Katzhendler, D. Gibson^*

^*Corresponding author for this work

School of Pharmacy

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

17 Scopus citations

Abstract

A new series of complexes of the type [PtAm₂LCl]⁺ (where Am = NH₃ or Am₂ = ethylenediamine and L is a monodentate AQ-Y-(CH₂)_n-NH₂, AQ = anthraquinone, Y = NH, O) was prepared and screened in vitro against P388 leukemia. These complexes displayed higher activities than the corresponding neutral PtAm₂L₂ 1:2 Pt:anthraquinone complexes but lower than the neutral diaminedichloro 1:1 complexes. The [Pt(en)LCl]⁺ complexes were significantly less active than the cis- and trans-[Pt(NH₃)₂LCl]⁺ complexes. The cis and trans isomers displayed similar activities. The complexes bearing the shorter linker chains were more active than those with longer chains. In vivo toxicity studies indicate that they are significantly less toxic than cis-DDP.

Original language	English
Pages (from-to)	593-598
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	26
Issue number	6
DOIs	https://doi.org/10.1016/0223-5234(91)90193-Q
State	Published - Sep 1991

Keywords

anthraquinone
platinum
structure-activity relationships
triaminemonochloro

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/0223-5234(91)90193-Q

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title = "Preparation, characterization and the anticancer activity of a novel series of triaminemonochloroplatinum(II) cations linked to anthraquinone intercalators",

abstract = "A new series of complexes of the type [PtAm2LCl]+ (where Am = NH3 or Am2 = ethylenediamine and L is a monodentate AQ-Y-(CH2)n-NH2, AQ = anthraquinone, Y = NH, O) was prepared and screened in vitro against P388 leukemia. These complexes displayed higher activities than the corresponding neutral PtAm2L2 1:2 Pt:anthraquinone complexes but lower than the neutral diaminedichloro 1:1 complexes. The [Pt(en)LCl]+ complexes were significantly less active than the cis- and trans-[Pt(NH3)2LCl]+ complexes. The cis and trans isomers displayed similar activities. The complexes bearing the shorter linker chains were more active than those with longer chains. In vivo toxicity studies indicate that they are significantly less toxic than cis-DDP.",

keywords = "anthraquinone, platinum, structure-activity relationships, triaminemonochloro",

author = "KF Gean and R. Ben-Shoshan and A. Ramu and I. Ringel and J. Katzhendler and D. Gibson",

year = "1991",

month = sep,

doi = "10.1016/0223-5234(91)90193-Q",

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AU - Gean, KF

AU - Ben-Shoshan, R.

AU - Ramu, A.

AU - Ringel, I.

AU - Katzhendler, J.

AU - Gibson, D.

PY - 1991/9

Y1 - 1991/9

N2 - A new series of complexes of the type [PtAm2LCl]+ (where Am = NH3 or Am2 = ethylenediamine and L is a monodentate AQ-Y-(CH2)n-NH2, AQ = anthraquinone, Y = NH, O) was prepared and screened in vitro against P388 leukemia. These complexes displayed higher activities than the corresponding neutral PtAm2L2 1:2 Pt:anthraquinone complexes but lower than the neutral diaminedichloro 1:1 complexes. The [Pt(en)LCl]+ complexes were significantly less active than the cis- and trans-[Pt(NH3)2LCl]+ complexes. The cis and trans isomers displayed similar activities. The complexes bearing the shorter linker chains were more active than those with longer chains. In vivo toxicity studies indicate that they are significantly less toxic than cis-DDP.

AB - A new series of complexes of the type [PtAm2LCl]+ (where Am = NH3 or Am2 = ethylenediamine and L is a monodentate AQ-Y-(CH2)n-NH2, AQ = anthraquinone, Y = NH, O) was prepared and screened in vitro against P388 leukemia. These complexes displayed higher activities than the corresponding neutral PtAm2L2 1:2 Pt:anthraquinone complexes but lower than the neutral diaminedichloro 1:1 complexes. The [Pt(en)LCl]+ complexes were significantly less active than the cis- and trans-[Pt(NH3)2LCl]+ complexes. The cis and trans isomers displayed similar activities. The complexes bearing the shorter linker chains were more active than those with longer chains. In vivo toxicity studies indicate that they are significantly less toxic than cis-DDP.

KW - anthraquinone

KW - platinum

KW - structure-activity relationships

KW - triaminemonochloro

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JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 6

ER -

Preparation, characterization and the anticancer activity of a novel series of triaminemonochloroplatinum(II) cations linked to anthraquinone intercalators

Abstract

Keywords

UN SDGs

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