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Bis-cyclometalated rhodium- and iridium-complexes with the 4,4′-dichloro-2,2′-bipyridine ligand. Evaluation of their photophysical properties and biological activity

Accepted Manuscript Research paper Bis- Cyclometalated Rhodium- and Iridium- Complexes With the 4,4’-Dichloro-2,2’-Bipyridine Ligand. Evaluation of their Photophysical Properties and Biological Activity Marion Graf, Yvonne Gothe, Nils Metzler-Nolte, Rafał Czerwieniec, Karlheinz Sünkel PII: DOI: Reference: S0020-1693(17)30247-5 http://dx.doi.org/10.1016/j.ica.2017.04.006 ICA 17510 To appear in: Inorganica Chimica Acta Received Date: Accepted Date: 29 March 2017 3 April 2017 Please cite this article as: M. Graf, Y. Gothe, N. Metzler-Nolte, R. Czerwieniec, K. Sünkel, Bis- Cyclometalated Rhodium- and Iridium- Complexes With the 4,4’-Dichloro-2,2’-Bipyridine Ligand. Evaluation of their Photophysical Properties and Biological Activity, Inorganica Chimica Acta (2017), doi: http://dx.doi.org/10.1016/ j.ica.2017.04.006 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Bis- Cyclometalated Rhodium- and Iridium- Complexes With the 4,4’-Dichloro-2,2’-Bipyridine Ligand. Evaluation of their Photophysical Properties and Biological Activity Dedicated to Prof. Hans-Christian Böttcher on the Occasion of his 60th Birthday Marion Grafa, Yvonne Gotheb, Nils Metzler-Nolteb, Rafał Czerwieniecc Karlheinz Sünkela* a Department of Chemistry, Ludwig Maximilian University of Munich, Butenandtstraße 5–13, 81377 Munich, Germany b c Ruhr University of Bochum, Universitätsstraße 150, 44801 Bochum, Germany Institute of Physical and Theoretical Chemistry University of Regensburg, Universitätsstraße 31, 93053 Regensburg, Germany ABSTRACT The synthesis and characterization of new cyclometalated complex salts [M(C^N)2(4,4’Cl2bpy)]PF6 (M = Rh and Ir; C^N = 2-(p-tolyl)pyridinato (1 and 2), 2-phenyl-5-chloropyridinato (3 and 4); 4,4’-Cl2bpy = 4,4’-dichloro-2,2’-bipyridine) is described. Compounds 1 - 4 were obtained by reaction of 4,4’-dichloro-2,2’-bipyridine with the complexes [{M(µCl)(C^N)2}2] (M = Rh, Ir) in refluxing CH2Cl2/MeOH mixtures. The molecular structures of compounds 1 and 4 were confirmed by X-ray diffraction. The Ir compounds show phosphorescence in PMMA film and in solution at ambient temperature. Furthermore, all compounds display significant cytotoxicity against human cancer cell lines with the IC50 values in the 0.4 - 2 µM range. KEYWORDS: Cyclometalated complexes; Rhodium; Iridium; phosphorescence; cytotoxicity __________________________________________________________________________ * Corresponding author. Tel.: +49 89218077773; fax: +49 89218077774 E-mail address: suenk@cup.uni-muenchen.de (K. Sünkel) 2 1. Introduction Bis-cyclometalated Ir(III) complexes play an important role in the development of modern optoelectronic technologies (e.g. organic light emitting diodes − OLEDs and lightemitting electrochemical cells − LEECs), biological labels, and chemical sensors [1]. It was found by several groups that as well for LEEC’s [2] as for sensoric applications [3], NLO materials[4] and bio-medical diagnostic and therapeutic studies [59] the use of water-soluble complexes of the type [M(C^N)2(N^N)]+ was particularly beneficial. Starting from the longknown compounds with M = Rh [10] and Ir [11], C^N = 2-phenylpyridinato (ppy) and N^N = 2,2’-bipyridine (bpy) or phenanthroline (phen), numerous studies were performed to elucidate the effects of various substituents on the photophysical and electrochemical properties of the complexes and how they influence the device performance in different applications [12-14]. Our group described a series of cyclometalated M(III) complexes (M = Rh, Ir) [15], including complexes containing biomolecules as the ancillary ligands [16]. Recently we found that the complexes [M(ptpy)2 ](ddpmp)]PF6 (M = Rh, Ir; ddmp = 4,7-dichloro-2,9-dimethyl-1,10-phenanthroline)), which contain chloro-substituents on the pyridine parts of the phenanthroline ligand, showed promising luminescence and cytotoxic properties [17]. In this paper we describe the synthesis and characterization of four new cyclometalated complex salts [M(C^N)2(4,4’-Cl2bpy)]PF6 which contain the structurally related 4,4’-dichloro-2,2’-bipyridine ligand, which was also studied before in a Rh(I) complex [18] for catalytic properties, a Ru(II) complex [19] as agent against tuberculosis or a Rh(III) complex [20] for indirect electrochemical cofactor regeneration. 2. Experimental 2.1. General considerations All manipulations were performed under an atmosphere of dry nitrogen using conventional Schlenk techniques. 4,4’-dichloro-2,2’-bipyridine (Aldrich), 2-(p-tolyl)pyridine (Aldrich), 5-chloro-2-phenyl-pyridine (Synchem) were used as received. [{M(µ-Cl)(C^N)2}2] (M = Rh, Ir) were prepared by adequately modified literature methods [15b, e]. NMR spectra were usually recorded in CD2Cl2 using a Jeol Eclipse 400 instrument operating at 400 MHz (1H) and 100 MHz (13C) respectively. Chemical shifts are given in ppm, referenced to the solvent signals at δ = 5.30 (1H) or 53.8 ppm (13C). Mass spectra were measured using a Jeol Mstation JMS 700 spectrometer. Elemental analyses (C, H, N) were performed by the Microanalytical Laboratory of the Department of Chemistry, LMU Munich, using a Heraeus Elementar Vario EL instrument. 3 Dulbecco’s Modified Eagle’s Medium (DMEM), containing 10% fetal calf serum, 1% penicillin and streptomycin, was used as growth medium. MCF-7 and HT-29 cells were detached from the wells with trypsin and EDTA, harvested by centrifugation and resuspended again in the cell culture medium. The assays were carried out on 96 well plates with 6000 (3000) cells per well for MCF-7 (HT-29, respectively). After 24 h of incubation at 37°C and 10% CO2, the cells were treated with the compounds 1 and 2 (with DMSO concentrations of 0.5%) with a final volume of 200 µl per well. For a negative control, one series of cells was left untreated. The cells were incubated for 48 h followed by adding 50 µl MTT (2.5 mg/ml). After an incubation time of 2 h, the medium was removed and 200 µl DMSO were added. The formazan crystals were dissolved and the absorption was measured at 550 nm, using a reference wavelength of 620 nm. Each test was repeated in quadruplicates in two independent experiments for each cell line. 2.2. Starting Materials 2.2.1. [{Ir(µ-Cl)(5-Cl-ppy)2}2] Yield: 440 mg (65.5 %). Anal. Calc. for C44H28Cl6 Ir2N4: C, 43.68; H, 2.33; N, 4.63 Found: C, 44.04; H, 2.57; N, 4.51 %. MS (FAB+): m/z = 1210.5 [M+H]+, 604.3 [M/2 +]. 1H NMR: δ 9.14 (d, J = 6.3 Hz, 4 H), 7.95 (d, J = 2.3 Hz, 4 H), 7.54 (dd, J =7.9/ 1.2 Hz, 4 H), 6.91 (dd, J = 6.3/ 2.3 Hz, 4H), 6.89-6.83 (m, 4H), 6.68 (td, J =7.5/ 1.3 Hz, 4 H), 5.95 (dd, J =7.8/ 1.1 Hz, 4H). 13C {1H} NMR (100 MHz, CDCl3): δ 169.7, 151.1, 145.3, 145.1, 142.7, 130.6, 130.1, 124.4, 122.4, 122.0, 119.1. 2.2.2. [{Rh(µ-Cl)(5-Cl-ppy)2}2] Yield: 45 mg (31.5 %). Anal. Calc. for C44H28Cl6N4Rh2 : C, 51.24; H, 2.74; N, 5.43. Found: C, 51.31; H, 3.06; N, 5.00 %. MS (FAB+): m/z = 1033 [M++2H], 516 [M/2+], 479 [M/2+-Cl]. 1H NMR: δ 9.09 (m, 4 H), 7.93 (d, J = 2.4 Hz, 4 H), 7.58 (dd, J = 7.8/ 1.4 Hz, 4 H), 6.92 (m, 4H), 6.88 (dt, J = 6.2/ 2.3 Hz, 4H), 6.74 (dt, J = 7.6/ 1.4 Hz, 4H), 5.96 (d, J = 7.2 Hz, 4H). 13C {1H} NMR: δ 166.68/ 166.66, 166.3 (d, JRhC = 36,6 Hz), 152.9, 145.9, 143.0, 132.4, 130.27/ 130.25, 124.50/ 124.49, 123.2, 122.66/122.65, 119.67/ 119.66. 2.3. Synthesis of [Rh(ptpy)2(4,4’Cl2bpy)]PF6 (1) To a solution of [{Rh(µ-Cl)(ptpy)2}2] (142 mg, 0.15 mmol) in 25 mL of CH2Cl2/ MeOH (1v: 1v) 4,4’-Cl2bpy = 4,4’-dichloro-2,2’-bipyridine (90 mg, 0.4 mmol) was added and the mixture refluxed with stirring for 2 h. After cooling to room temperature, KPF6 (70 mg, 4 0.4 mmol) was added. The solvent was removed to dryness in vacuo and the residue dissolved in dichloromethane and chromatographed on alumina with CH2 Cl2/ acetone (9:1) as the eluent. The solution was evaporated to dryness and the residue was redissolved in 5 ml of dichloromethane and 1 was crystallized by slow diffusion of n-hexane. Yield: 142 mg (58.4%). Anal. Calc. for C34H26Cl2 F6N4PRh: C, 50.45; H, 3.24; N, 6.92. Found: C, 50.78; H, 3.48; N, 6.50 %. MS (FAB+): m/z = 663.4 [M+] complex cation. 1H NMR (400 MHz, CD2Cl2): δ 8.36 (d, J= 1.9 Hz, 2 H), 7.95 (d, J= 5.8 Hz, 2 H), 7.91 (d, J= 7.8 Hz, 2 H), 7.88- 7.83 (m, 2 H), 7.68 (d, J= 7.9 Hz, 2 H), 7.50 (dd, J= 5.8/ 1.8 Hz, 2 H), 7.46 (d, J= 5.8 Hz, 2 H), 7.07- 7.01 (m, 2H), 6.96 (d, J= 8.4 Hz, 2 H), 6.09 (s, 2H), 2.13 (s, 6 H). 13C {1H} NMR (400 MHz, CD2Cl2): δ 166.4 (d, JRhC = 32Hz), 165.18/165.17, 154.9, 151.4, 148.8, 148.7, 141.47/141.46, 141.2, 138.8, 133.7, 128.8, 125.3, 125.00, 124.99, 123.39/ 123.38, 120.17/120.15, 21.6. 2.4. Synthesis of [Ir(ptpy)2(4,4’-Cl2bpy)]PF6 (2) To a solution of [{Ir(µ-Cl)(ptpy)2}2] (169 mg, 0.15 mmol) in 25 mL of a mixture of CH2Cl2/MeOH (1:1) the ligand 4,4’-Cl2bpy = 4,4’-dichloro-2,2’-bipyridine (90 mg, 0.4 mmol) was added and the mixture refluxed with stirring for 2 h. After cooling to room temperature KPF6 (70 mg, 0.38 mmol) was added. The solvent was removed in vacuo and the residue was dissolved in dichloromethane and chromatographed on alumina with CH2Cl2/acetone (9:1) as the eluent. The solution was evaporated to dryness and the residue redissolved in 5 ml of dichloromethane. The product was precipitated by slow diffusion of hexane. Suitable crystals for X-ray diffraction were obtained by slow diffusion of hexane into a solution of dichloromethane/chloroform at room temperature. Yield: 142 mg (52.7 %). Anal. Calc. for C34H26Cl2F6IrN4P: C, 45.44; H, 2.92; N, 6.23. Found: C, 44.91; H, 3.09; N, 5.87 %. MS (FAB+): m/z = 753.3 [M+] complex cation. 1HNMR: δ 8.36 (d, J= 2 Hz, 2 H), 7.90 (m, 4 H), 7.75 (m, 2 H), 7.60 (d, J= 12 Hz, 2 H), 7.44 (m, 4 H), 6.97 (m, 2 H), 6.88 (d, J= 8 Hz, 2 H), 6.05 (s, 2 H), 2.13 (s, 6 H). 13C {1H} NMR: δ 167.6, 166.0, 151.5, 149.0 148.4, 147.8, 141.4, 140.9, 138.3, 132.3, 132.3, 129.1, 125.3, 124.9, 124.0, 123.0, 119.6, 21.5. 2.5. Synthesis of [Rh(5-Cl-ppy)2(4,4’Cl2bpy)]PF6 (3) 5 To a solution of [{Rh(µ-Cl)(5-Cl-ppy)2}2] (155 mg, 0.15 mmol) in 20 mL of a mixture of CH2Cl2/MeOH (1:1), the ligand 4,4’-Cl2bpy = 4,4’-dichloro-2,2’-bipyridine (68 mg, 0.3 mmol) was added and the mixture was stirred and refluxed for 2 hours. After cooling to room temperature KPF6 (74 mg, 0.4 mmol) was added. The solvent was removed in vacuo and the residue was dissolved in dichloromethane and chromatographed on alumina with CH2Cl2/acetone (9:1) as the eluent. Crystals were obtained by slow diffusion of isohexane into a solution in dichloromethane/chloroform at room temperature. Yield: 141.3 mg (55 %). Anal. Calc. for C32H20Cl4F6N4PRh: C, 45.21; H, 2.37; N, 6.59. Found: C, 45.21; H, 2.72; N, 6.43 %. MS (FAB+): m/z = 705.2 [M+] complex cation. 1 H NMR: δ= 8.39 (d, J= 2.0 Hz, 2 H), 7.95 (d, J= 2.2 Hz, 2 H), 7.89 (d, J= 5.7 Hz, 2 H), 7.74 (d, J= 7.3 Hz, 2 H), 7.51 (dd, J= 5.8/ 2.0 Hz, 2 H), 7.46 (d, J= 6.2 Hz, 2 H), 7.16 (t, J= 7.5 Hz, 2 H), 7.12 (dd, J= 6.2/ 2.2 Hz, 2 H), 7.08-7.02 (m, 2 H), 6.36 (d, J= 7.6 Hz, 2 H). 13 C {1H} NMR : δ= 166.5 (d, JRhC= 32 Hz), 166.03/166.01, 154.8, 151.2, 149.9, 149.0, 147.5, 142.8, 133.1, 131.63/131.61, 129.0, 125.5, 125.4, 124.5, 124.4, 120.82/120.81. 2.6. Synthesis of [Ir(5-Cl-ppy)2(4,4’-Cl2bpy)]PF6 (4) To a solution of [{Ir(µ-Cl)(5-Cl-ppy)2}2] (181.5 mg, 0.15 mmol) in 20 mL of a mixture of CH2Cl2/ MeOH (1:1), the ligand 4,4’-Cl2bpy = 4,4’-dichloro-2,2’-bipyridine (68 mg, 0.3 mmol) was added and the mixture was stirred and refluxed for 2 hours. After cooling to room temperature KPF6 (70 mg, 0.38 mmol) was added. The solvent was removed in vacuo and the residue was dissolved in dichloromethane and chromatographed on alumina with CH2Cl2/ acetone (9:1) as the eluent. Suitable crystals for X-ray diffraction were obtained by slow diffusion of isohexane into a solution in dichloromethane/chloroform at room temperature. Yield: 160.5 mg (57 %). Anal. Calc. for C32H20Cl4F6IrN4P: C, 40.91; H, 2.15; N, 5.96. Found: C, 40.61; H, 2.33; N, 5.69 %. MS (FAB+): m/z = 793.4 [M+] complex cation. 1 H-NMR: δ = 8.41 (d, J= 2.1 Hz, 2 H), 7.94 (d, J = 2.2 Hz, 2 H), 7.86 (d, J = 5.9 Hz, 2 H), 7.70 (dd, J = 7.9/ 1.1 Hz, 2 H), 7.50 (dd, J= 5.9/ 2.1 Hz, 2 H), 7.47 (dd, J= 6.3/ 0.5 Hz, 2 H), 7.15- 7.05 (m, 4 H), 6.99 (td, J= 7.4/ 1.3 Hz, 2 H), 6.33 (dd, J= 7.6/ 0.7 Hz, 2H). 13 C {1H} NMR: δ= 168.8, 156.0, 151.4, 149.5, 149.0, 148.3, 146.9, 142.5, 131.8, 131.6, 129.3, 125.7, 125.5, 124.0, 123.3, 120.3. 6 2.7. X-ray structural determinations A suitable single crystal of 1 was selected by means of a polarization microscope, mounted on the tip of a glass fiber, and investigated on a BRUKER D8 Venture diffractometer using Mo-Kα radiation (λ = 0.71073 Å). The crystal turned out to be a racemic twin, containing two symmetry-independent molecules in the asymmetric unit. The intensities were corrected for absorption by the semi-empirical multiscan method (SADABS). The structure was solved by direct methods (SIR 97) using a HKLF4 file and refined by full-matrix least-squares calculations on F2 (SHELXL-2014/7) using a HKLF5 file with BASF= 0.268, as implemented in the software package WINGX. [21] Refinement turned out to be rather difficult, as the compound co-crystallized with CH2Cl2, MeOH and water, which could be localized (however, severely disordered) and refined using several restraints. Even then, analysis by PLATON showed the presence of 4.8% solvent accessible voids. Anisotropic displacement parameters were refined for all non-hydrogen atoms except the carbon and oxygen atoms of the disordered solvent molecules. Crystals of 4 suitable for an X-ray diffraction study were grown from CH2Cl2/CHCl3/hexane solutions. Data collection, structure solution (SIR 97) and refinement (SHELXL-2014/7) could be performed without any problems. There were neither co-crystallized solvents nor any residual solvent accessible voids. Details of the crystal data, data collection, structure solution, and refinement parameters are summarized in Table 1. 2.8. Photophysical Measurements. UV-Vis absorption spectra were recorded with a Varian Cary 300 double beam spectrometer. Luminescence spectra were measured with a Horiba Jobin Yvon Fluorolog 3 steady-state fluorescence spectrometer. For decay time measurements a PicoQuant LDH-P-C375 pulsed diode laser (λexc = 372 nm, pulse width 100 ps) was applied as the excitation source. The emission signal was detected with a cooled photomultiplier attached to a FAST ComTec multichannel scalar card with a time resolution of 250 ps. Photoluminescence quantum yields were determined with a Hamamatsu C9920-02 system equipped with a Spectralon integrating sphere. Diluted solutions (c ≈ 10 −5 M−1) in dichloromethane (CH2Cl2) were degassed by several freeze-pump-thaw cycles (p = 1×10−5 mbar). Polymer films containing about 0.1 weight% of the Ir complex were obtained by dissolving the emitter and 7 poly(methyl methacrylate) (PMMA) in dichloromethane and spin-coating this solutions onto quartz glass substrates. PMMA films were measured under continuous flushing with nitrogen. 8 Table 1:Crystal data and structure refinement details for 1 and 3. Compound 1 4 Empirical formula C35.75H30.5Cl4.5F6N4OPRh C32H20Cl4F6IrN4P Formula weight 939.55 939.49 Temperature [K] 100(2) 173(2) Crystal system Monoclinic Space group P 21 P 21/n a [Å] 11.6660(6) 9.4737(3) b 25.4895(14) 13.8553(4 c 14.1754(8) Å 24.5688(8) 93.879(2). 93.509(3) 4205.5(4) 3218.88(17) 2x2 4 Density (calc., [g/cm ]) 1.484 1.939 Absorption coefficient 0.790 mm-1 4.597 F(000) 1886 1816 Crystal size [mm3] 0.08 x 0.04 x 0.03 0.279 x 0.118 x 0.07 Theta range for data collection 2.881 to 26.453°. 4.31 to 26.37°. Index ranges -14≤h≤14, 0≤k≤31, 0≤l≤17 -11≤h≤11, -15≤k≤17, -19≤l≤30 Reflections collected 11822 20539 Independent reflections 11822 6559 [R(int) = 0.0426] Completeness 99.7 % 99.6 % Max. and min. transmission 0.7454 and 0.693 1 and 0.84257 Data / restraints / parameters 11822 / 17 / 949 6559 / 0 / 433 Goodness-of-fit on F2 1.125 1.086 Final R indices [I>2sigma(I)] R1 = 0.0540, wR2 = 0.1271 R1 = 0.0529, wR2 = 0.1325 R indices (all data) R1 = 0.0631, wR2 = 0.1323 R1 = 0.0618, wR2 = 0.1389 Absolute structure parameter 0.05(5) - Largest diff. peak and hole [e.Å-3] 1.381 and -0.626 4.992 and -1.278 Unit cell dimensions ß [°] 3 Volume [Å ] Z 3 2.9. Computational Methodology. Molecular geometries and electronic structures of [Rh(ptpy)2(4,4’-Cl2bpy)]PF6 and [Ir(ptpy)2(4,4’-Cl2bpy)]PF6 were calculated using the density functional theory (DFT) with the hybrid gradient corrected correlation functional B3LYP [22]. The Ahlrichs split-valence basis set SVP [23] was applied for atoms C, H, N, and Cl and the quadruple-zeta quality basis 9 set QZVP [24] was used for Rh and Ir atoms. Inner-core electrons of Rh and Ir were substituted with relativistic effective core potentials. [25] TD-DFT calculations for [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) were performed in the optimized ground state geometry using the same B3LYP functional and basis sets. Ten lowest singlet and triplet excitations were computed. All computations were carried out using the Gaussian 09 program package.[26] 2.10. Cell culture and cytotoxicity. Dulbecco’s Modified Eagle’s Medium (DMEM), containing 10% FCS, 1% penicillin and streptomycin, was used as growth medium. MCF-7 and HT-29 cells were detached from the wells with trypsin and EDTA, harvested by centrifugation and re-suspended in cell culture medium. The assays have been carried out on 96 well plates with 6000 cells per well for both cell lines. After 24 h of incubation at 37°C and 10% CO2, the cells were treated with the compounds (with DMSO concentrations of 0.5%) with a final volume of 200 µl per well. For the negative control, one series of cells was left untreated. The cells were incubated for 48 h followed by adding 50 µl MTT (2.5 mg/ml). After an incubation time of 2 h, the medium was removed and 200 µl DMSO were added. The formazan crystals were dissolved and the absorption was measured at 550 nm, using a reference wavelength of 620 nm. Each test was repeated in triplicates or quadruplicates in at least three independent experiments for each cell line. 3. Results and discussion 3.1. Synthesis and characterization of compounds The cyclometalating ligands 2-para-tolyl-pyridine (“Hptpy”) and 5-Chloro-2phenylpyridine (“HClppy”) were used for the synthesis of the chloro-bridged dimers [{M(µCl)(C^N)2}2] (M = Rh, Ir; C^N= ptpy, ClPppy) starting from the corresponding M(I) complexes [{M(µ-Cl)(coe)2}2] by an oxidative addition reaction as described previously [15b, e]. Subsequently, the preparation of the cationic mononuclear title complexes was started by cleavage of these dimeric compounds by the chelating ligand 4,4’-Cl2bpy = 4,4’-dichloro2,2’-bipyridine in a refluxing mixture of dichloromethane/methanol. The primarily formed chloride salts [M(C^N)2(4,4’-Cl2bpy)]Cl yielded after metatheses with KPF6 the hexafluorophosphate derivatives 1 – 4 (see Scheme 1). All compounds were obtained as yellow crystals in good yields and were characterized by elemental analyses, 1H and 13C NMR 10 spectroscopy, mass spectrometry and additionally for 1 and 4 by single crystal X-ray diffraction studies. Scheme 1: Synthesis of compounds 1–4 3.2. Crystal and molecular structures of 1 and 4 Figure 2: Molecular Structure of the cation Figure 1: Molecular Structure of the cation of compound 4; shown is the Λ isomer of compound 1; shown is the isomer with ∆ configuration ORTEP drawings of both compounds can be seen in Figures 1 and 2. Compound 1 crystallized unfortunately as a racemic twin with disordered solvent molecules in approximate stoichiometry (1)4(CH2Cl2)5(MeOH)2(H2O)2. The unit cell contains two symmetryindependent molecules of 1, one with ∆- configuration and one with Λ configuration on Rh. 11 The nitrogen atoms of the cyclometalating ligands are in a mutual trans- configuration, as usually observed. The bond parameters (in Å and °) involving the metal atoms are collected in Table 2. As can be seen there, these parameters are for both independent molecules identical within the 2σ criterion. The bonds from rhodium to the bpy nitrogen atoms are by ca. 0.1Å longer than to the nitrogen atoms of the cyclometallating ligands, which is presumably due to the trans influence of the Rh-C bonds. Very similar parameters were observed in the related thienyl-pyridine complex [Rh(thpy)2(bpy)]Cl, (comp.”A” in Table 2) [10c]. The planes of the two pyridine rings of the bpy ligand are slightly twisted (4.4° and 8.0°). Compound 4 crystallizes with no solvents in the centrosymmetric space group P21/n with only one independent molecule in the asymmetric unit. Again, the nitrogen atoms of the cyclometallating ligands are in mutual trans configuration. Bond parameters around the central iridium atom are collected again in Table 2. Again, the bond lengths from the metal to the bpy nitrogen atoms are longer than those to the Clppy nitrogen atoms, but somewhat surprising, they are actually slightly shorter than the corresponding bond lengths of the rhodium compound. However, similar distances and angles were reported for the related [Ir(ppy)2(bpy)]PF6 (comp. “B” in Table 2) [2c]. The planes of the two halves of the bipy ligand are again slightly twisted by 7°, while in B this torsion angle amounts only to 1.4°. Table 2: Bond geometries around the metal atoms in 1 and 4 and two related complexes. M-Nbpy 1 (mol. 1) 2.158(11) 2.153(10) 1 (mol. 2) 2.156(10) 2.175(9) A 2.145(3) 2.138(4) 2.136(6) 4 2.136(6) 2.129 B 2.136 M-NC^N M-CC^N (N-M-N)bpy (N-M-C)C^N (N-M-N’)C^N C-M-Nbpy 2.023(10) 2.061(10) 2.050(10) 2.038(11) 2.055(4) 2.065(4) 2.054(6) 2.021(6) 2.047 2.042 1.998(12) 2.012(10) 2.013(10) 1.988(14) 1.984(4) 1.993(5) 2.031(8) 2.015(7) 2.024 2.004 75.5(4) 80.5(5) 81.6(4) 82.2(5) 81.3(5) 80.7(2) 81.1(2) 79.7(3) 80.1(3) 80.68 80.02 75.0(4) 76.7(1) 76.1(2) 76.20 173.3(4) 172.9(4) 170.7(1) 172.9(3) 172.09 173.8(6) 171.8(5) 171.6(5) 174.0(5) 173.6(2) 173.7(2) 172.8(3) 175.6(3) 171.92 171.90 3.3. Photophysical properties UV-Vis absorption spectra were studied in dichloromethane (c = 0.05 mM) at room temperature. Absorption maxima for both Rh and Ir complexes are listed in Table 3 (below). The respective spectra of [Rh(ptpy)2(4,4’-Cl2bpy)]PF6 (1) and [Ir(ptpy)2(4,4’-Cl2bpy)]PF6 (2) are shown in Fig. 3. With reference to previous studies on related complexes [1c, 17, 27–31] the higher-energy intense bands occurring at λabs ≤ 330 (with maximum molar absorption coefficients ε in the order of 104 M−1cm−1) nm are assigned to spin-allowed ligand-centered π 12 → π* transitions of the ptpy and 4,4’-Cl2bpy ligands. In the lower energy region, between 330 and 400 nm for [Rh(ptpy)2(4,4’-Cl2bpy)]PF6 (1) and 330 – 450 nm for [Ir(ptpy)2(4,4’Cl2bpy)]PF6 (2), respectively, weaker absorption bands (ε in the order of several thousand M−1cm−1) are observed. Since such absorptions are not displayed by the free ligands ptpyH and 4,4’-Cl2bpy, the long-wavelength absorption bands of the Rh and Ir complexes are assigned to metal-to-ligand charge-transfer (MLCT) transitions involving the occupied dπ orbitals of the metals (4dπ(Rh) and 5d π(Ir) in [Rh(ptpy)2(4,4’-Cl2bpy)]PF6 (1) and [Ir(ptpy)2(4,4’-Cl2bpy)]PF6 (2), respectively) and empty π* orbitals of the ptpy and 4,4’Cl2bpy ligands. The significant red-shift of the MLCT absorptions in the Ir complex as compared to the Rh congener is readily accounted for the higher energy of the occupied d orbitals of the 5d 6 ion Ir3+ than in the 4d6 ion Rh3+, respectively. The above assignments are further supported by results of the TD-DFT calculations. In particular, the frontier orbitals of [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) drawn in Fig. 3 involve different regions of the molecule. As analyzed in Table 3, The HOMO is largely composed of a 5dπ atomic orbital of Ir with significant admixtures of the π (ptpy) character and the LUMO (π*) is largely centered on the 4,4’-Cl2bpy ligand. Since the lowest energy transitions S0→T1 and S0→S1 result mainly from the HOMO→LUMO excitation, distinct charge-transfer character (5d π(Ir)→ π*(4,4’-Cl2bpy)) of the lowest excited states is predicted. Table 3. Percent contributions of Ir, ptpy, and 4,4’-Cl2bpy to selected highest occupied lowest virtual molecular orbitals of [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2). The Mulliken population analysis was performed for the ground-state Kohn-Sham orbitals resulting from the B3LYP/{SVP+QZVP(ECP)} DFT calculations using the Chemissian computer program [32 Orbital Energy (eV) Ir (%) ptpy1 (%) ptpy2 (%) 4,4’-Cl2bpy (%) HOMO – 5 -9.018 40 27 27 6 HOMO – 4 -8.920 64 15 15 5 HOMO – 3 -8.874 28 33 33 5 HOMO – 2 -8.661 16 41 41 - HOMO – 1 -8.468 5 47 47 - HOMO -7.942 35 32 32 2 LUMO -5.439 3 - - 96 LUMO + 1 -4.616 3 2 2 93 LUMO + 2 -4.347 1 2 2 95 13 LUMO + 3 -4.222 5 47 47 1 LUMO + 4 -4.142 4 46 46 4 LUMO + 5 -3.718 3 47 47 4 Table 4. Vertical transition energies, oscillator strengths, and orbital character of three lowest energy electronic transitions of [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) resulting from TD-DFT computations on the B3LYP/[SVP+QZVP(ECP)] level of theory. Transition Energy Oscillator /eV strength Main contributions S0→T1 1.809 0 HOMO→LUMO (96 %) S0→T2 2.406 0 HOMO-5→LUMO (64 %) HOMO-3→LUMO (16 %) HOMO-1→LUMO (16 %) S0→T3 2.474 0 HOMO-4→LUMO (55 %) HOMO-2→LUMO (40 %) S0→S1 1.837 0.0002 HOMO→LUMO (98 %) S0→S2 2.509 0.0105 HOMO-1→LUMO (98 %) S0→S3 2.580 0.0006 HOMO-4→LUMO (61 %) HOMO-2→LUMO (38 %) Natural transition orbitals [33] hole electron 14 Figure 3. UV-Vis absorption and room-temperature luminescence spectra of [M(ptpy)2(4,4’Cl2bpy)]PF6. M = Rh (1): Blue solid line (solvent CH2Cl2). M = Ir (2): Black dashed lines (solvent CH2Cl2) and dotted line (PMMA matrix). The iridium complexes [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) and [Ir(5-Cl-ppy)2(4,4’-Cl2bpy)]+ (4) are luminescent in solution and in organic polymer matrices. (Fig. 3 and Table 5) In dichloromethane at ambient temperature, they show weak red emission centered at 660 nm (2) and 643 nm (4) with the quantum yields φPL of 3 and 6 %, respectively. The decay times τ are 60 and 50 ns, respectively. In poly(methyl methacrylate) (PMMA), the emissions with maxima at λem = 580 nm (2) and 560 nm (4) are significantly blue shifted relative to the liquid solution. The quantum yields and emission decay times increase by about 10 times to φPL = 32 % and τ = 900 ns for [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) and φPL = 60 % and τ = 950 ns for, [Ir(5-Clppy)2(4,4’-Cl2bpy)]+ (4), respectively. The relatively small radiative rates calculated according to kr = φPL/τ, being kr = 3.6 × 105 s−1 for 2 and kr = 6.3 × 10 5 s−1 for 4, respectively, point to a spin forbidden character of the corresponding electronic transitions. Thus, the emitting state is assigned as the lowest triplet state 3MLCT (5dπ(Ir)→ π*(4,4’-Cl2bpy)). However, the kr values are still relatively high as for phosphorescence. A corresponding allowedness is results from strong spin-orbit coupling of the lowest triplet state to the higher 1MLCT singlet states. (cf. [1c ,34].) Rigidochromic effects similar to those described above for [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) and [Ir(5-Cl-ppy)2(4,4’-Cl2bpy)]+ (4), such as the spectral blue shift and increase of φPL and τ when liquid solution (CH2Cl2) is replaced with a rigid polymer matrix (PMMA), were already reported for analogous luminescent iridium complexes. [17,29,31,35,36] Thus, the observed emission enhancement in rigid PMMA matrix as compared to the liquid CH2Cl2 solution can be accounted for different electrostatic interactions of the 3MLCT-excited molecule with the induced dipole moments in its close surrounding. In solution, the solutesolvent rearrangements lead to significant stabilization of the 3MLCT excited state and, thus, to a lower emission energy (longer wavelength; λem = 660 nm (for 2) in CH2 Cl2). As a consequence, vibrational coupling between the emitting 3MLCT state and the ground state increases leading, according to the energy-gap law [1c ,37], to more effective non-radiative relaxation manifested by distinctly lower φPL and τem values. On the contrary, in PMMA such reorganizations are largely suppressed. Thus, non-radiative relaxation of the apparently blue- 15 shifted emission (λem = 580 nm (for 2) in PMMA) becomes less important and the φPL and τem values remain large. Table 5. UV-vis absorption and luminescence dataa for complexes 1 – 4 at ambient temperature. Complex 1 2 3 4 365 (0.9); 266 (4.1) - 390 (0.8); 273 (4.6) 660 373 (0.9); 266 (5.5) - 380 (0.8); 275 (4.6) 643 φPL [%] (CH2Cl2) - 3 - 6 τem [ns] (CH2Cl2) - 60 - 50 λem [nm] (PMMA) - 580 - 560 φPL [%] (PMMA) - 32 - 60 τem [ns] (PMMA) - 900 - 950 λabs [nm], ε [104 M−1cm−1] in parentheses. (CH2Cl2) λem [nm] (CH2Cl2) a) λabs = absorption maximum, ε = molar absorption coefficient, λem = emission maximum, φPL = emission quantum yield, and τem = emission decay time, respectively. 3.5. Biological activity. Several cyclometalated Ir(III) and Rh(III) complexes not only show strong luminescence, but also manifest encouraging antiproliferative properties both in vitro and in vivo. For this reason, the antiproliferative activity of the complexes towards the cancer cell lines MCF-7 (human breast adenocarcinoma) and HT-29 (colon adenocarcinoma) has been evaluated using the MTT assay. The resulting IC50 values are shown in Table 4. Table 4 Antiproliferative effects of complexes 1 – 4 in MCF-7 and HT-29 cells. IC50 values are expressed as means [µM] (± standard deviation) of three independent experiments. Numbers are reported to two relevant digits in all cases for consistency, thus resulting in apparently different precision IC50/µM Compound HT-29 MCF-7 [Rh(ptpy)2(Cl2-bpy)]PF6 (1) 0.41 ± 0.21 2.37 ± 0.81 [Ir(ptpy)2(Cl2-bpy)]PF6 (2) 0.55 ± 0.19 1.43 ± 0.21 16 [Rh(Cl-ptpy)2(Cl2-bpy)]PF6 (3) 0.663 ± 0.060 1.68 ± 0.52 [Ir(Cl-ptpy)2(Cl2-bpy)]PF6 (4) 0.609 ± 0.098 2.00 ± 0.52 Cisplatin 4.14 ± 0.31 23.03 ± 0.25 It is found that all complexes exhibit appreciable cytotoxicity against the two cell lines with IC50 values ranging from 0.4 µM to 2.4 µM. The highest activity was observed for 1, which exhibits a 10-fold higher activity towards both cell lines than the clinical drug cisplatin. In a previous work, we have investigated similar cyclometalated complexes, in which the bipyridine moiety was substituted by a phenanthroline unit.[17] In accordance with these previously tested compounds, the MCF-7 cells show lower sensitivity to the compound treatments than the HT-29 cells. The complexes show similar cytotoxic activity compared to their phenanthroline analogues with the exception of having slightly higher IC50 values for MCF-7 cells. All in all, all compounds exhibit a strong cytotoxic activity in the high nanomolar/ low micromolar range with no significant difference in the cytotoxic behavior between the two metals in this specific ligand system. These initial biological studies illustrate the high antiproliferative potential of our complexes emphasising the suitability of cyclometalated iridium and rhodium complexes as new promising anti-cancer agents. 4. Conclusions The syntheses, photophysical properties, and biological activity of four new biscyclometalated cationic complexes [M(C^N)2(4,4’-Cl2bpy)]PF6 (M = Rh; Ir; C^N = ptpy, Clppy) are reported. Crystal and molecular structures of the new complexes were confirmed by X-ray crystal structure determination Iridium complexes 2 and 4 are luminescent in solution and in polymer matrices at ambient temperature. The emission assigned to a 3MLCT state strongly depends on the environment. In a rigid polymer matrix (PMMA), [Ir(ptpy)2(4,4’-Cl2bpy)]+ (2) and [Ir(5-Cl-ppy)2(4,4’-Cl2bpy)]+ (4) show moderately strong yellow luminescence whereas in solution (CH2Cl2) the emission is significantly red shifted. The emission quantum yield φPL and decay time τem values are significantly larger in rigid PMMA than in liquid solution due to different efficiency of non-radiative relaxations to the ground state. This rigidochromic behavior is accounted for distinctly different stabilization of 17 the 3MLCT-excited state in flexible solution and quasi-solid polymer films. All compounds exhibit cytotoxic effects towards two cell lines (HT29 and MCF-7). Acknowledgments The authors are grateful to the Department of Chemistry of the Ludwig Maximilians University Munich for support. P. Mayer is acknowledged for collecting the X-ray crystal data and Ms. Mahboubeh Jamshidi (University Regensburg) is acknowledged for her assistance with photophysical measurements. The Johnson Matthey plc, Reading, UK, is gratefully acknowledged for a generous loan of hydrated iridium chloride. Supplementary material CCDC-1528482 (1) and –1528483 (4) contain the supplementary crystallographic data for this paper. These data can be obtained free of charge from The Cambridge Crystallographic Data Centre via http://www.ccdc.cam.ac.uk/data_request/cif. References [1] [2] [3] [4] (a) C.-H. Lin, Y.-C. Chiu, Y. Chi, Y.-T. Tao, L.-S. Liao, M.-R. Tseng, G.-H. Lee, Organometallics 31 (2012) 4349 and references therein; (b) S.-K. Leung, K.Y. Kwok, K.Y. Zhang, K. K.-W. Lo, Inorg. Chem. 49 (2010) 4984 and references therein; (c) H. Yersin, A. F. Rausch, R. 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Chem. 87 (1983) 952. 20 Highlights • 4 new bis-cyclometalated Rh and Ir complexes with 4,4‘-Cl2BiPy are described • Crystal structures of [M(C^N)2(4,4’Cl2BiPy)] (M=Rh,Ir) are reported • All complexes show antiproliferative activity against certain cancer cells • The Ir complexes are strong yellow emitters in PMMA matrix