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Is the Aromatic Fragment of Piano‐Stool Ruthenium Compounds an Essential Feature for Anticancer Activity? The Development of New Ru II ‐[9]aneS 3 Analogues (Eur. J. Inorg. Chem. 17/2005)
Author(s) -
Serli Barbara,
Zangrando Ennio,
Gianferrara Teresa,
Scolaro Claudine,
Dyson Paul J.,
Bergamo Alberta,
Alessio Enzo
Publication year - 2005
Publication title -
european journal of inorganic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.667
H-Index - 136
eISSN - 1099-0682
pISSN - 1434-1948
DOI - 10.1002/ejic.200590036
Subject(s) - chemistry , ruthenium , ligand (biochemistry) , stereochemistry , steric effects , chelation , group 2 organometallic chemistry , denticity , medicinal chemistry , metal , molecule , organic chemistry , biochemistry , receptor , catalysis
The cover picture shows the X‐ray structures of some new half‐sandwich (or piano‐stool) Ru II ‐[9]aneS 3 complexes ([9]aneS 3 = 1,3,7‐trithiacyclononane) against a background of cells in culture. The complexes of the type [RuCl 2 (L)([9]aneS 3 )], [RuCl(L) 2 ([9]aneS 3 )][CF 3 SO 3 ], and [Ru(dmsoS)(L) 2 ([9]aneS 3 )][CF 3 SO 3 ] 2 (L = 1,3,5‐triaza‐7‐phosphaadamantane, PTA; (L) 2 = 2 PTA or chelating N‐ligand) were prepared from Ru‐[9]aneS 3 ‐dmso precursors and structurally characterized, both in solution and in the solid state. Some of them are analogues of known cytotoxic half‐sandwich Ru II (η 6 ‐arene) organometallic compounds of the type [RuCl(en)(η 6 ‐arene)][PF 6 ] and [RuCl 2 (PTA)(η 6 ‐arene)], in which the aromatic fragment is replaced by the sulfur macrocycle [9]aneS 3 while the rest of the coordination sphere is left unchanged. Preliminary in vitro tests performed on some complexes against the mouse adenocarcinoma cancer cell line (TS/A) and the human mammary normal cell line (HBL‐100) showed that, in general, the Ru‐[9]aneS 3 compounds have a cytotoxicity comparable to that of the corresponding organometallic analogues. These results suggest that the aromatic fragment of the piano‐stool Ru II compounds is not an essential feature for the in vitro anticancer activity, and it might be effectively replaced by another face‐capping ligand with a low steric demand, such as [9]aneS 3 . Details are discussed in the article by E. Alessio et al. on p. 3423 ff. This work was performed within the framework of COST Action D20, a collaboration between WG 0001 and WG 0005.