Ruthenium complexes offer potential reduced toxicity compared to current platinum anticancer drugs. 1,2,3,4-tetrahydrisoquinoline amino alcohol ligands were synthesised, characterised and coordinated to an organometallic Ru(II) centre. These complexes were evaluated for activity against the cancer cell lines MCF-7, A549 and MDA-MB-231 as well as for toxicity in the normal cell line MDBK. They were observed to be moderately active against only the MCF-7 cells with the best IC₅₀ value of 34 μM for the cis-diastereomeric complex C4. They also displayed excellent selectivity by being relatively inactive against the normal MDBK cell line with SI values ranging from 2.3 to 7.4.
Keywords: 1,2,3,4-tetrahydrisoquinoline; 1,8- diazabicycloundec-7-ene; A549; ATR; Anticancer; Cbz-Cl; DBU; DIPEA; ESI-QTOF; FA; HRMS; IC(50); LiAlH(4); MCF-7; MDA-MB-231; MDBK; MDR; Madin–Darby bovine kidney; Me(2)SO(4); Michigan cancer foundation-7; N,N; N,N-diisopropylethylamine; N,O; N-donor; Na(2)SO(4); NaBH(4); Pd/C; R(f); Ru(II); Ruthenium; SAR; SI; SOCl(2); TBDMS; TEA; TIQ; Tetrahydroisoquinoline; amino alcohol; atm; atmosphere; attenuated total reflectance; benzyl chloroformate; diamine; dimethyl sulfate; electrospray ionization quadrupole time of flight; formic acid; half maximal inhibitory concentration; high resolution mass spectrometry; human breast epithelial adenocarcinoma; human lung epithelial adenocarcinoma; lithium aluminium hydride; micro molar; multidrug resistance; nitrogen donor; palladium on carbon; part per million; ppm; retention factor; ruthenium(II); selectivity index; sodium borohydride; sodium sulfate; structure activity relationship; tert-butyl dimethyl silyl; thionyl chloride; triethylamine; μM.
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