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. 1986 Sep 15;238(3):757–763. doi: 10.1042/bj2380757

Binuclear platinum (II)-terpyridine complexes. A new class of bifunctional DNA-intercalating agent.

W D McFadyen, L P Wakelin, I A Roos, B L Hillcoat
PMCID: PMC1147201  PMID: 3800959

Abstract

A series of binuclear DNA-binding ligands was prepared by linking two (2,2':6',2"-terpyridine)platinum(II) moieties via alpha omega-dithiols of the type HS-[CH2]n-SH where n = 4-10. A monomeric analogue was also synthesized. Compounds were characterized by elemental analysis and electronic and n.m.r. spectroscopy. Viscometric measurements with sonicated rod-like DNA fragments and covalently closed circular DNA were performed to investigate the mode of binding of these agents. The ligands with n = 5 and 6 function as bis intercalators and form a single 'base-pair sandwich' in violation of neighbour-exclusion binding. Bifunctional reaction occurs for the ligand with n = 7, whereas the ligands with n = 8 and 10 show a preference for mixed monofunctional/bifunctional binding. The data do not permit definitive assignment of the binding mode of the ligands with n = 4 and 9. All compounds are growth-inhibitory against mouse leukaemia L1210 cells in culture with IC50 values in the range 2-14 microM.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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