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Titolo:
Synthesis, characterization, and cytotoxicity of trifunctional dinuclear platinum complexes: Comparison of effects of geometry and polyfunctionality on biological activity
Autore:
Qu, Y; Rauter, H; Fontes, APS; Bandarage, R; Kelland, LR; Farrell, N;
Indirizzi:
Virginia Commonwealth Univ, Dept Chem, Richmond, VA 23284 USA Virginia Commonwealth Univ Richmond VA USA 23284 , Richmond, VA 23284 USA Inst Canc Res, CRC Ctr Canc Therapeut, Sutton SM2 5NG, Surrey, England Inst Canc Res Sutton Surrey England SM2 5NG tton SM2 5NG, Surrey, England
Titolo Testata:
JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 16, volume: 43, anno: 2000,
pagine: 3189 - 3192
SICI:
0022-2623(20000810)43:16<3189:SCACOT>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
INTRASTRAND CROSS-LINKS; CELL-LINES; DNA; BINDING; D(GPG); NMR;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Farrell, N Virginia Commonwealth Univ, Dept Chem, Med Coll Virginia Campus, Richmond,VA 23284 USA Virginia Commonwealth Univ Med Coll Virginia CampusRichmond VA USA 23284
Citazione:
Y. Qu et al., "Synthesis, characterization, and cytotoxicity of trifunctional dinuclear platinum complexes: Comparison of effects of geometry and polyfunctionality on biological activity", J MED CHEM, 43(16), 2000, pp. 3189-3192

Abstract

The synthesis of two new isomeric trifunctional dinuclear platinum complexes of formula [{PtCl(NH3)(2)}mu-NH2(CH2)(6)NH2-{PtCl2(NH3)}](+) (1,2/c,c and 1,2/t,c) is reported. Their biological activity in selected human tumor cell lines sensitive and resistant to CDDP (cisplatin, cis-[Pt(NH3)(2)Cl-2])is described and compared with the profile for their bifunctional analogues, [{cis/trans-PtCl(NH3)(2)}(2)mu-NH2(CH2)(6)NH2](2+). The trifunctional dinuclear platinum complexes showed a unique profile of cytotoxicity against human cancer cell lines, with low resistance factors in A2780, CH1, and 41Mcell. lines. The resistance factor is dependent on the geometry of the Pt coordination spheres - suggesting that these may be associated with DNA-binding modes. Retention of activity against CDDP-resistant cell lines and a different spectrum of activity compared to CDDP and also within different classes of polynuclear platinum complexes suggest that not only are they mechanistically different from mononuclear platinum complexes but also each individual class of polynuclear platinum structure may have its own unique character.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/09/20 alle ore 17:14:59