Novel C,N-chelate platinum(II) antitumor complexes bearing a lipophilic ethisterone pendant

J Ruiz; V Rodriguez; N Cutillas; A Espinosa; Michael Hannon

doi:10.1016/j.jinorgbio.2010.12.005

Novel C,N-chelate platinum(II) antitumor complexes bearing a lipophilic ethisterone pendant

J Ruiz, V Rodriguez, N Cutillas, A Espinosa, Michael Hannon

Chemistry

Research output: Contribution to journal › Article

46 Citations (Scopus)

Abstract

The novel steroidal carrier ligand 17-alpha[4'-ethynyl-dimethylbenzylamine]-17-beta-testosterone (ET-dmba 1) and the steroid - C,N-chelate platinum(II) derivatives [Pt(ET-dmba)Cl(L)] (L = DMSO (2) and PTA (3; PTA = 1,3,5-triaza-7-phosphaadamantane)) have been prepared. Values of IC50 were calculated for the new platinum complexes 2 and 3 against a panel of human tumor cell lines representative of ovarian (A2780 and A2780cisR) and breast cancers (T47D). At 48 h incubation time complexes 2 and 3 show very low resistance factors (RF of

Original language	English
Pages (from-to)	525-531
Number of pages	7
Journal	Journal of Inorganic Biochemistry
Volume	105
Issue number	4
DOIs	https://doi.org/10.1016/j.jinorgbio.2010.12.005
Publication status	Published - 1 Apr 2011

Keywords

Cytotoxicity
Lipophilicity
Steroidal derivative
DNA
Platinum complexes

UN SDGs

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

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10.1016/j.jinorgbio.2010.12.005

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title = "Novel C,N-chelate platinum(II) antitumor complexes bearing a lipophilic ethisterone pendant",

abstract = "The novel steroidal carrier ligand 17-alpha[4'-ethynyl-dimethylbenzylamine]-17-beta-testosterone (ET-dmba 1) and the steroid - C,N-chelate platinum(II) derivatives [Pt(ET-dmba)Cl(L)] (L = DMSO (2) and PTA (3; PTA = 1,3,5-triaza-7-phosphaadamantane)) have been prepared. Values of IC50 were calculated for the new platinum complexes 2 and 3 against a panel of human tumor cell lines representative of ovarian (A2780 and A2780cisR) and breast cancers (T47D). At 48 h incubation time complexes 2 and 3 show very low resistance factors (RF of ",

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author = "J Ruiz and V Rodriguez and N Cutillas and A Espinosa and Michael Hannon",

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TY - JOUR

T1 - Novel C,N-chelate platinum(II) antitumor complexes bearing a lipophilic ethisterone pendant

AU - Ruiz, J

AU - Rodriguez, V

AU - Cutillas, N

AU - Espinosa, A

AU - Hannon, Michael

PY - 2011/4/1

Y1 - 2011/4/1

N2 - The novel steroidal carrier ligand 17-alpha[4'-ethynyl-dimethylbenzylamine]-17-beta-testosterone (ET-dmba 1) and the steroid - C,N-chelate platinum(II) derivatives [Pt(ET-dmba)Cl(L)] (L = DMSO (2) and PTA (3; PTA = 1,3,5-triaza-7-phosphaadamantane)) have been prepared. Values of IC50 were calculated for the new platinum complexes 2 and 3 against a panel of human tumor cell lines representative of ovarian (A2780 and A2780cisR) and breast cancers (T47D). At 48 h incubation time complexes 2 and 3 show very low resistance factors (RF of

AB - The novel steroidal carrier ligand 17-alpha[4'-ethynyl-dimethylbenzylamine]-17-beta-testosterone (ET-dmba 1) and the steroid - C,N-chelate platinum(II) derivatives [Pt(ET-dmba)Cl(L)] (L = DMSO (2) and PTA (3; PTA = 1,3,5-triaza-7-phosphaadamantane)) have been prepared. Values of IC50 were calculated for the new platinum complexes 2 and 3 against a panel of human tumor cell lines representative of ovarian (A2780 and A2780cisR) and breast cancers (T47D). At 48 h incubation time complexes 2 and 3 show very low resistance factors (RF of

KW - Cytotoxicity

KW - Lipophilicity

KW - Steroidal derivative

KW - DNA

KW - Platinum complexes

U2 - 10.1016/j.jinorgbio.2010.12.005

DO - 10.1016/j.jinorgbio.2010.12.005

M3 - Article

C2 - 21334280

VL - 105

SP - 525

EP - 531

JO - Journal of Inorganic Biochemistry

JF - Journal of Inorganic Biochemistry

IS - 4

ER -

Novel C,N-chelate platinum(II) antitumor complexes bearing a lipophilic ethisterone pendant

Abstract

Keywords

UN SDGs

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