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Titolo:
X-ray structure of cytotoxic trans-[PtCl2(dimethylamine) (isopropylamine)]: Interstrand cross-link efficiency, DNA sequence specificity, and inhibition of the B-Z transition
Autore:
Perez, JM; Montero, EI; Gonzalez, AM; Solans, X; Font-Bardia, M; Fuertes, MA; Alonso, C; Navarro-Ranninger, C;
Indirizzi:
Univ Autonoma Madrid, Dept Quim Inorgan, E-28049 Madrid, Spain Univ Autonoma Madrid Madrid Spain E-28049 Inorgan, E-28049 Madrid, Spain Univ Autonoma Madrid, CSIC, Ctr Biol Mol Severo Ochoa, E-28049 Madrid, Spain Univ Autonoma Madrid Madrid Spain E-28049 o Ochoa, E-28049 Madrid, Spain Univ Barcelona, E-08028 Barcelona, Spain Univ Barcelona Barcelona Spain E-08028 rcelona, E-08028 Barcelona, Spain
Titolo Testata:
JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 12, volume: 43, anno: 2000,
pagine: 2411 - 2418
SICI:
0022-2623(20000615)43:12<2411:XSOCT(>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
PLATINUM ANTITUMOR COMPLEXES; HANDED Z-DNA; ANTICANCER DRUGS; PLANAR LIGANDS; ACTIVATION; CRYSTAL; CELLS; TRANS-; REACTIVITY; CHEMISTRY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Navarro-Ranninger, C Univ Autonoma Madrid, Dept Quim Inorgan, E-28049 Madrid, Spain Univ Autonoma Madrid Madrid Spain E-28049 id, Spain
Citazione:
J.M. Perez et al., "X-ray structure of cytotoxic trans-[PtCl2(dimethylamine) (isopropylamine)]: Interstrand cross-link efficiency, DNA sequence specificity, and inhibition of the B-Z transition", J MED CHEM, 43(12), 2000, pp. 2411-2418

Abstract

We report here the X-ray structure of cytotoxic trans-[PtCl2(dimethylamine)(isopmpylamine)]. This trans-platinum compound crystallizes in the monoclinic system, with Z = 8, in the spatial group C2/c with unit cell parametersa = 19.862(17) Angstrom, b = 6.581(3) Angstrom, c = 18.563(3) Angstrom, alpha = 90 degrees, beta = 119.16(3)degrees, gamma = 90 degrees, V = 2119(2) Angstrom(3), rho = 2.321 Mg/m(3), R = 0.0505, and R-w = 0.1166 on the basisof 2339 independent reflections. To our knowledge this is the first reportof the crystal structure of a biologically active trans-platinum compound containing different aliphatic amines. The DNA binding mode of trans-[PtCl2(dimethylamine)(isopropylamine)] may be a consequence of the spatial disposition of the dimethylamine and isopropylamine ligands around the trans-Pt(II) center. We have found that trans-[PtCl2(dimethylamine)(isopropylamine)] readily forms DNA interstrand cross-links. In addition, the compound shows binding affinity toward alternating purine-pyrimidine sequences and inhibits the B-Z-transition. These particular DNA binding properties might be related to the capacity of trans-[PtCl2(dimethylamine)(isopropylamine)] for inducing some selective killing in a H-ras overexpresssing cell line.

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Documento generato il 05/04/20 alle ore 03:45:21