(2016). Highly water-soluble cyclopentadienyl and indenyl molybdenum(II) complexes -second generation of molybdenum-based cytotoxic agents. European Journal of Inorganic Chemistry, 2016Chemistry, (4), 519-529. doi:10.1002 This article may be used for non-commercial purposes in accordance With Wiley-VCH Terms and Conditions for self-archiving". Ondřej Mrózek, [a] Lucie Šebestová, [b] Jaromír Vinklárek,* [a] Martina Řezáčová, [c] Aleš Eisner, [b] Zdeňka Růžičková, [a] and Jan Honzíček [d] Abstract [BF4]2 were determined by the X-ray crystallography. All synthesized compounds exhibit increased activity against human leukemia cell lines MOLT-4 and HL-60. They are about one order of magnitude more active than cisplatin. This study has proven that modification of the outer coordination sphere of molybdenum complexes has a strong impact on their activity and may be successfully used for a design of novel highly cytotoxic active species.
A series of vanadocene complexes [Cp′2V(L)][OTf]2 (Cp′ = η5‐C5H5, η5‐C5H4Me; L = phen, 5‐NO2‐phen, 5‐NH2‐phen, 4,7‐Ph2‐phen) was prepared and characterized by mass spectrometry and EPR spectroscopy. Structures of two complexes that contain an N,N′‐chelating ligand, [(η5‐C5H4Me)2V(phen)][OTf]2·0.5Me2CO and [(η5‐C5H5)2V(5‐NH2‐phen)][OTf]2, and the triflate intermediate [(η5‐C5H5)2V(OTf)2] were further confirmed by X‐ray diffraction analysis. The cytotoxicity study has shown that complexes that contain phenanthroline ligands have considerably higher in vitro activity toward human leukemia cells MOLT‐4 and HL‐60 than their parent dichlorides ([Cp′2VCl2]). The high activity of these complexes coheres with their higher stability in various aqueous media. This study has further shown that substitution of chloride ligands in the vanadocene dichloride has a considerably higher effect on cytotoxicity than expected on the basis of established mechanistic rules.
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