Anthraquinone intercalators as carrier molecules for second-generation platinum anticancer drugs

D. Gibson; I. Binyamin; M. Haj; I. Ringel; A. Ramu; J. Katzhendler

doi:10.1016/S0223-5234(99)80068-3

Anthraquinone intercalators as carrier molecules for second-generation platinum anticancer drugs

D. Gibson^*, I. Binyamin, M. Haj, I. Ringel, A. Ramu, J. Katzhendler

^*Corresponding author for this work

School of Pharmacy

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

31 Scopus citations

Abstract

A series of complexes PtAm₂L [where Am₂ = (NH₃)₂, ethylenediamine(en), 1,2-diaminocyclohexane (DACH) or (NH₃)(c-C₆H₁₁NH₂) and where L is a bidentate 1,1-dicarboxylate ligand tethered to 1- aminoanthraquinone by various spacers] was prepared and screened in vitro against P388 leukemia cells. The free ligands displayed moderate activity and the corresponding platinum complexes were tenfold more active. The nature of the linker chain does not seem to affect the potency of the complexes. The potency depends on the nature of the inert amine ligand [NH₃ > DACH > en]. The low aqueous solubility of these complexes prevented any in vivo studies and the preparation of water soluble analogs is currently under way.

Original language	English
Pages (from-to)	823-831
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	32
Issue number	10
DOIs	https://doi.org/10.1016/S0223-5234(99)80068-3
State	Published - Oct 1997

Keywords

Anthraquinone
Anticancer
Carrier
Intercalator
Platinum

UN SDGs

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

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10.1016/S0223-5234(99)80068-3

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title = "Anthraquinone intercalators as carrier molecules for second-generation platinum anticancer drugs",

abstract = "A series of complexes PtAm2L [where Am2 = (NH3)2, ethylenediamine(en), 1,2-diaminocyclohexane (DACH) or (NH3)(c-C6H11NH2) and where L is a bidentate 1,1-dicarboxylate ligand tethered to 1- aminoanthraquinone by various spacers] was prepared and screened in vitro against P388 leukemia cells. The free ligands displayed moderate activity and the corresponding platinum complexes were tenfold more active. The nature of the linker chain does not seem to affect the potency of the complexes. The potency depends on the nature of the inert amine ligand [NH3 > DACH > en]. The low aqueous solubility of these complexes prevented any in vivo studies and the preparation of water soluble analogs is currently under way.",

keywords = "Anthraquinone, Anticancer, Carrier, Intercalator, Platinum",

author = "D. Gibson and I. Binyamin and M. Haj and I. Ringel and A. Ramu and J. Katzhendler",

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AU - Gibson, D.

AU - Binyamin, I.

AU - Haj, M.

AU - Ringel, I.

AU - Ramu, A.

AU - Katzhendler, J.

PY - 1997/10

Y1 - 1997/10

N2 - A series of complexes PtAm2L [where Am2 = (NH3)2, ethylenediamine(en), 1,2-diaminocyclohexane (DACH) or (NH3)(c-C6H11NH2) and where L is a bidentate 1,1-dicarboxylate ligand tethered to 1- aminoanthraquinone by various spacers] was prepared and screened in vitro against P388 leukemia cells. The free ligands displayed moderate activity and the corresponding platinum complexes were tenfold more active. The nature of the linker chain does not seem to affect the potency of the complexes. The potency depends on the nature of the inert amine ligand [NH3 > DACH > en]. The low aqueous solubility of these complexes prevented any in vivo studies and the preparation of water soluble analogs is currently under way.

AB - A series of complexes PtAm2L [where Am2 = (NH3)2, ethylenediamine(en), 1,2-diaminocyclohexane (DACH) or (NH3)(c-C6H11NH2) and where L is a bidentate 1,1-dicarboxylate ligand tethered to 1- aminoanthraquinone by various spacers] was prepared and screened in vitro against P388 leukemia cells. The free ligands displayed moderate activity and the corresponding platinum complexes were tenfold more active. The nature of the linker chain does not seem to affect the potency of the complexes. The potency depends on the nature of the inert amine ligand [NH3 > DACH > en]. The low aqueous solubility of these complexes prevented any in vivo studies and the preparation of water soluble analogs is currently under way.

KW - Anthraquinone

KW - Anticancer

KW - Carrier

KW - Intercalator

KW - Platinum

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Anthraquinone intercalators as carrier molecules for second-generation platinum anticancer drugs

Abstract

Keywords

UN SDGs

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