Enhanced cytotoxicity of indenyl molybdenum() compounds bearing a thiophene function

A series of six indenyl molybdenum compounds bearing a thiophenyl function in the side chain were prepared and characterized by analytical and spectroscopic methods. The structures of [(η 5 -C 9 H 6 CH 2 C 4 H 3 S)(η 3 -C 3 H 5 )Mo(CO) 2 ] and [(η 5 -C 9 H 6 CH 2 C 4 H 3 S)Mo(CO) 2 (bpy)][BF 4 ] wer...

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Published in:Dalton transactions : an international journal of inorganic chemistry 2019-08, Vol.48 (3), p.11361-11373
Main Authors: Mrózek, Ond ej, Melounková, Lucie, Dostál, Libor, Císa ová, Ivana, Eisner, Aleš, Havelek, Radim, Peterová, Eva, Honzí ek, Jan, Vinklárek, Jaromír
Format: Article
Language:English
Subjects:
Bearing
Biological activity
Biotechnology
Chelation
Crystallography
Ligands
Molybdenum
Molybdenum compounds
Numbering schemes
Single crystals
Toxicity
Tumors
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Summary:A series of six indenyl molybdenum compounds bearing a thiophenyl function in the side chain were prepared and characterized by analytical and spectroscopic methods. The structures of [(η 5 -C 9 H 6 CH 2 C 4 H 3 S)(η 3 -C 3 H 5 )Mo(CO) 2 ] and [(η 5 -C 9 H 6 CH 2 C 4 H 3 S)Mo(CO) 2 (bpy)][BF 4 ] were determined by single-crystal X-ray diffraction. The compounds bearing N , N -chelating ligands exhibit increased cytotoxic activity against human leukemia cell lines MOLT-4; up to two orders of magnitude lower IC 50 values were observed compared to analogues with unsubstituted indenyl, which clearly demonstrates the strong effect of the indenyl ligand modification on the biological activity of the molybdenum( ii ) compounds. The highest cytostatic potential was observed for the complex bearing 4,7-diphenyl-1,10-phenanthtoline [(η 5 -C 9 H 6 CH 2 C 4 H 3 S)Mo(CO) 2 (Ph 2 phen)][BF 4 ] with IC 50 (MOLT-4) = 0.19 ± 0.02 μM. Detailed regulation of the molecular and cellular mechanism by this derivative was investigated on the lung carcinoma cell line A549 and compared with the lung fibroblast cell line MRC-5. Rather unusual differences in the effects on tumor and non-tumor cell lines provide a unique insight into the cytostatic action of molybdenum( ii ) complexes. New indenyl molybdenum( ii ) compounds with improved cytotoxic properties were synthesized and evaluated in lung cancer cells A549.
ISSN:1477-9226
1477-9234
DOI:10.1039/c9dt01698h