SYNTHESIS, CHARACTERIZATION AND CYTOTOXIC ACTIVITY OF SOME Ru (II) COMPLEXES (original) (raw)
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Synthesis and cytotoxic activity of some mononuclear Ru(II) Complexes
A series of mononuclear Ru(II) complexes of the type [Ru(T)2(S)]2+, where T=2,2'-bipyridine/1,10-phenanthroline and S= 4-N-(CH3)2-btsz, 4-OH-btsz, 4-N-(CH3)2-binh have been prepared and characterized by UV-Vis, IR, 1H-NMR, FAB-Mass spectroscopy, and elemental analysis. The title complexes were subjected to in vitro cytotoxic activity against human cancer cell line Molt 4/C8, CEM and murine tumor cell line L 1210. Invitro evaluation of these ruthenium complexes revealed cytotoxic activity from 1.30 to 50μM against Molt 4/C8, 0.30 to 24 μM aginst CEM, 0.87 to 41 μM against L1210 cell proliferation, depending on the nature of the compound
Synthesis, antineoplastic and cytotoxic activities of some mononuclear Ru (II) complexes
Journal of Enzyme Inhibition and Medicinal Chemistry, 2010
A series of mononuclear Ru(II) complexes of the type [Ru(S)(2)(K)](2+), where S = 1,10-phenanthroline/2,2'-bipyridine and K = 4-OH-btsz, 4-CH(3)-btsz, 3,4-di-OCH(3)-btsz, 4-OH-binh, 4-CH(3)-binh, 3,4-di-OCH(3)-binh, were prepared and characterized by elemental analysis, FTIR, (1)H-NMR, and mass spectroscopy. The complexes displayed metal-ligand charge transfer (MLCT) transitions in the visible region. These ligands formed bidentate octahedral ruthenium complexes. The title complexes were evaluated for their in vivo anticancer activity against a transplantable murine tumor cell line, Ehrlisch's ascites carcinoma (EAC), and in vitro cytotoxic activity against human cancer cell lines Molt 4/C(8) and CEM and murine tumor cell line L1210. The ruthenium complexes showed promising biological activity especially in decreasing tumor volume and viable ascites cell counts. Treatment with these complexes prolonged the life span of mice bearing EAC tumors by 10-52%. In vitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.21 to 24 muM against Molt 4/C(8), 0.16 to 19 microM against CEM, and 0.75 to 32 microM against L1210.
Medicinal Chemistry Research, 2016
The synthesis and characterization of ruthenium complexes (Ru-1–Ru-6) of the type [Ru(R)2(K)]2+ (where R = 1,10-phenanthroline/2,2′-bipyridyl and K = acetyl coumarin-inh, pyrazole-tch, acetyl coumarin-tsz, are described. These ligands form bidentate octahedral ruthenium complexes. The in vitro cytotoxic activities of the complexes measurement against the human cancer Tlymphocyte cell lines. In vitro evaluation of these title complexes revealed cytotoxicity from 0.34 to 1.4 µg/mL against CEM, 0.28 to 1.8 µg/mL against L1210, 0.44 to 2.5 µg/mL against Molt4/C8, 0.98 to 1.6 µg/mL against HL60, and 0.66 to 1.4 µg/mL against BEL7402. Ruthenium complexes Ru-5 & Ru-6 showed that quite significant anticancer activities over standard drugs.
The synthesis and spectroscopic characterization of ruthenium complexes (R-1 to R-8) of the type [Ru(A) 2 (B)], (where A = 1,10-phenanthroline/2,2 0 -bipyridine and B = 3,4,5-tri-OCH 3 -DPC, 4-CH 3 -DPC, 4-N-(CH 3 ) 2 -DPC, 4-NO 2 -DPC are described. These ligands form bidentate octahedral ruthenium complexes. The title complexes were subjected to in vitro cytotoxic activity measurements against the human cancer T-lymphocyte cell lines MTT assay. In vitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.24 to 1.4 mg/mL against CEM, 0.44 to 1.9 mg/mL against Molt4/C8, 0.28 to 1.5 mg/mL against L1210, 0.24 to 0.98 mg/mL against HL60, and 0.25 to 1.2 mg/mL against BEL7402, depending the nature of the compound.
Synthesis and anticancer activity of certain mononuclear Ru (II) Complexes
Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
Bis(1,10-phenanthroline/2,2 0 -bipyridine) ruthenium(II)complexes containing TCP, TTZ OPBI, and BTSC ligands (where, TCP ¼ 1-thiocarbamoyl-3,5-diphenyl-2-pyrazoline,TTZ ¼ 2-(3,5-diphenyl-4,5-dihydropyrazol-1-yl)-4-phenylthiazole, OPBI ¼ 2-hydroxyphenyl benzimidazole and BTSC ¼ benzoin thiosemicarbazone) have been prepared and characterized. The spectral data suggested that the ligands were coordinated with the metal through nitrogen, sulfur and oxygen atoms. The target complexes were tested in vivo for anticancer activity against transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC). All these complexes increased the life span of the EAC-bearing mice, decreased their tumor volume and viable ascitic cell count as well as improved Hb, RBC and WBC counts. These results suggest that the Ru(II) complexes exhibit significant antitumor activity in EAC-bearing mice. It was also observed that the ruthenium complexes protected red blood cells from 2,2 0 -azo-bis(2-methylpropionamidine) dihydrochloride (AAPH)-induced hemolysis. The inhibitory effect was dose-dependent at a concentration of 20 -120 mg/ml.
Synthesis, anticancer, and cytotoxic activities of some mononuclear Ru (II) compounds
Bioorganic & medicinal …, 2007
The synthesis and characterization of ruthenium compounds (Ru1-Ru12) of the type [Ru(S)(2)(K)], (where S=1,10-phenanthroline/2,2'-bipyridine and K=itsz, MeO-btsz, 4-Cl-btsz, 2-Cl-btsz, 2-F-btsz, hfc and itsz=isatin-3-thiosemicarbazone, MeO-btsz=1-(4'-methoxy-benzyl)-thiosemicarbazone, hfc=2-{[3-chloro-4-fluoro-phenylimino]methyl}phenol, 4-Cl-btsz=1-(4'-chlorobenzyl)-thiosemicarbazone, 2-Cl-btsz=1-(2'-chloro benzyl)-thiosemicarbazone, 2-F-btsz=1-(2'-fluorobenzyl)-thiosemicarbazone) are described. These ligands form bidentate octahedral ruthenium compounds. The title compounds were subjected to in vivo anticancer activity against a transplantable murine tumor cell line Ehrlich's Ascites Carcinoma (EAC) and in vitro cytotoxic activity against human cancer cell line Molt 4/C8, CEM and murine tumor cell line L1210. Ruthenium compounds (Ru1-Ru12) showed promising biological activity especially in decreasing tumor volume and viable ascites cell counts. Treatment with these compounds prolonged the life span of mice bearing EAC tumor by 10-43%. In vitro evaluation of these ruthenium compounds revealed cytotoxic activity from 0.24 to 27 microM against Molt 4/C8, 0.27 to 48 microM against CEM, and 0.94 to 248 microM against L1210. Their ligands alone failed to show cytotoxic activity at the concentrations tested (68-405 microM).
Molecules
Two new complexes of Ru(II) with mixed ligands were prepared: [Ru(bpy)2smp](PF6) (1) and [Ru(phen)2smp](PF6) (2), in which smp = sulfamethoxypyridazine; bpy = 2,2′-bipyridine; phen = 1,10-phenanthroline. The complexes have been characterized by elemental and conductivity analyses; infrared, NMR, and electrospray ionization mass spectroscopies; and X-ray diffraction of single crystal. Structural analyses reveal a distorted octahedral geometry around Ru(II) that is bound to two bpy (in 1) or two phen (in 2) via their two heterocyclic nitrogens and to two nitrogen atoms from sulfamethoxypyridazine—one of the methoxypyridazine ring and the sulfonamidic nitrogen, which is deprotonated. Both complexes inhibit the growth of chronic myelogenous leukemia cells. The interaction of the complexes with bovine serum albumin and DNA is described. DNA footprinting using an oligonucleotide as substrate showed the complexes’ preference for thymine base rich sites. It is worth notifying that the compl...