title: Anticancer activity of ruthenium(II) arene complexes bearing 1,2,3,4-tetrahydroisoquinoline amino alcohol ligands.
abstract: 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.
authors.affiliation: Catalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-Natal, Durban 4000, KwaZulu-Natal, South Africa.
authors.forename: Madichaba P
authors.initials: MP
authors.lastname: Chelopo
authors.forename: Sachin A
authors.initials: SA
authors.lastname: Pawar
authors.forename: Mxolisi K
authors.initials: MK
authors.lastname: Sokhela
authors.forename: Thavendran
authors.initials: T
authors.lastname: Govender
authors.forename: Hendrik G
authors.initials: HG
authors.lastname: Kruger
authors.forename: Glenn E M
authors.initials: GE
authors.lastname: Maguire
mesh_terms: D000605:Amino Alcohols / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D008024:Ligands; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D000605:Amino Alcohols; D000970:Antineoplastic Agents; D008024:Ligands; D009942:Organometallic Compounds; D012428:Ruthenium
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