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1.
Iqbal Choudhary M Shahab Alam M Atta-Ur-Rahman Yousuf S Wu YC Lin AS Shaheen F 《Steroids》2011,76(14):1554-1559
Pregnenolone (1) was used as a template to develop new anticancer compounds. Ring-D modification of 1 resulted in the synthesis of benzylidenes 2-17, pyrazolines 18-76, pyrazoles 85-91, hydrazones 77-84, and oximes 92-107 derivatives. The structure of compound 107 was also deduced through single crystal X-ray diffraction studies. The inclusion of furanyl and pyridyl rings to pregnenolone skeleton increases the cytotoxicity of all compounds significantly. Among benzylidene derivatives, only heterocyclic enone 8 (IC50 = 0.74 μM/mL against HepG2), and 17 (IC50 = 4.49 μM/mL against HepG2, IC50 = 5.01 μM/mL against MDA-MB-230 cancer cell line) exhibited a significant activity. The cytotoxicity data of pyrazoline derivatives 18-76 revealed that only furanyl bearing pyrazolines 40, 42-44, 48, and 49 exhibited significant activities. While all (O-carboxymethyl) oximes, hydazones, and pyrazoles derivatives of pregnenolone did not show any significant activity against both the cell lines. Thus the furanyl bearing enone 8 (IC50 = 0.74 μM/mL against HepG2), and its pyrazoline derivative 48 (IC50 = 0.91 μM/mL against MDA-MB-230 cancer cell lines) were identified as the most active compounds in all derivatives of pregnenolone. 相似文献
2.
Dong Y Nakagawa-Goto K Lai CY Morris-Natschke SL Bastow KF Lee KH 《Bioorganic & medicinal chemistry letters》2011,21(8):2341-2344
4-Amino-2H-benzo[h]chromen-2-one (ABO) and 4-amino-7,8,9,10-tetrahydro-2H-benzo[h]chromen-2-one (ATBO) analogs were found to be significant in vitro anticancer agents in our previous research. Our continuing study has now discovered a new simplified (monocyclic rather than tricyclic) class of cytotoxic agents, 4-amino-2H-pyran-2-one (APO) analogs. By incorporating various substituents on the pyranone ring, we have established preliminary structure-activity relationships (SAR). Analogs 19, 20, 23, and 26-30 displayed significant tumor cell growth inhibitory activity in vitro. The most active compound 27 exhibited ED50 values of 0.059-0.090 μM. 相似文献
3.
Abdellatif KR Huang Z Chowdhury MA Kaufman S Knaus EE 《Bioorganic & medicinal chemistry letters》2011,21(13):3951-3956
A novel hybrid nitric oxide-releasing anti-inflammatory (AI) ester prodrug (NONO-coxib 14) wherein an O2-acetoxymethyl 1-(2-carboxypyrrolidin-1-yl)diazen-1-ium-1,2-diolate (O2-acetoxymethyl PROLI/NO) NO-donor moiety was covalently coupled to the CH2OH group of 3-(4-hydroxymethylphenyl)-4-(4-methylsulfonylphenyl)-5H-furan-2-one (12), was synthesized. The prodrug 14 released a low amount of NO (4.2%) upon incubation with phosphate buffer (PBS) at pH 7.4 which was significantly higher (34.8% of the theoretical maximal release of two molecules of NO/molecule of the parent hybrid ester prodrug) upon incubation in the presence of rat serum. These incubation studies suggest that both NO and the parent compound 12 would be released from the prodrug 14 upon in vivo cleavage by non-specific serum esterases. The prodrug ester 14 is a selective COX-2 inhibitor that exhibited AI activity (ED50 = 72.2 mmol/kg po) between that of the reference drugs celecoxib (ED50 = 30.9 μmol/kg po) and ibuprofen (ED50 = 327 μmol/kg po). The NO donor compound 14 exhibited enhanced inhibition of phenylephrine-induced vasoconstriction of isolated mesenteric arteries compared with that observed under control conditions. These studies indicate hybrid ester AI/NO donor prodrugs (NONO-coxibs) constitutes a plausible drug design concept targeted toward the development of selective COX-2 inhibitory AI drugs that are devoid of adverse cardiovascular effects. 相似文献
4.
The nuclearity, bonding and H-bonded networks of copper(I) halide complexes with thiophene-2-carbaldehyde thiosemicarbazones {(C4H3S)HC2N3-N(H)-C1(S)N1HR} are influenced by R substituents at N1 atom. Thiophene-2-carbaldehyde-N1-methyl thiosemicarbazone (HttscMe) or thiophene-2-carbaldehyde-N1-ethyl thiosemicarbazone (HttscEt) have yielded halogen-bridged dinuclear complexes, [Cu2(μ-X)2(η1-S-Htsc)2(Ph3P)2] (Htsc, X: HttscMe, I, 1; Br, 2; Cl, 3; HttscEt, I, 4; Br, 5; Cl, 6), while thiophene-2-carbaldehyde-N1-phenyl thiosemicarbazone (HttscPh) has yielded mononuclear complexes, [CuX(η1-S-HttscPh)2] (X, I, 7a; Br 8; Cl, 9) and a sulfur bridged dinuclear complex, [Cu2(μ-S-HttscPh)2(η1-S-HttscPh)2I2] 7b co-existing with 7a in the same unit cell. These results are in contrast to S-bridged dimers [Cu2(μ-S-Httsc)2(η1-Br)2(Ph3P)2] · 2H2O and [Cu2(μ-S-Httsc)2(η1-Cl)2(Ph3P)2] · 2CH3CN obtained for R = H and X = Cl, Br (Httsc = thiophene-2-carbaldehyde thiosemicarbazone) as reported earlier. The intermolecular CHPh?π interaction in 1-3 (2.797 Å, 1; 3.264 Å, 2; 3.257 Å, 3) have formed linear polymers, whereas the CHPh?X and N3?HCH interactions in 4-6 (2.791, 2.69 Å, 5; 2.776, 2.745 Å, 6, respectively) have led to the formation of H-bonded 2D polymer. The PhN1H?π, interactions (2.547 Å, 8, 2.599 Å, 9) have formed H-bonded dimers only. The Cu?Cu separations are 3.221-3.404 Å (1-6). 相似文献
5.
Vijaya Laxmi S Thirupathi Reddy Y Suresh Kuarm B Narsimha Reddy P Crooks PA Rajitha B 《Bioorganic & medicinal chemistry letters》2011,21(14):4329-4331
A novel series of barbiturate and thiobarbiturate analogs of 2-benzoyl-3-methyl-5-oxo-5H-furo[3,2-g]chromene-6-carbaldehydes (3a-g and 4a-d, respectively) and 6-methyl-4,8-dioxo-4,8-dihydropyrano[3,2-g]chromenes (7a-c), were synthesized and evaluated for their antitubercular activities against Mycobacterium tuberculosis H37RV, and cytotoxicity (CC50) in the VERO cell MABA assay. The results indicate that the furanochromene series of compounds (3a-g and 4a-d) showed only weak to moderate antitubercular activity. However, the pyranochromene analog 7b showed good antitubercular activity (IC90: 5.9 μg/mL) and cytotoxicity (CC50: 14.27 μg/mL). The antitubercular activity of 7b was superior to the antituberculosis drug, pyrazinamide (PZA; IC90: >20 μg/mL). Analog 7b was considered to be a lead compound for subsequent structural optimization. 相似文献
6.
So Young Lee 《Inorganica chimica acta》2009,362(4):1047-3853
Two isomeric dibenzo-O2S2 macrocycles L1 and L2 have been synthesised and their coordination chemistry towards palladium(II) has been investigated. Two-step approaches via reactions of 1:1-type complexes, [cis-Cl2LPd] (1a: L = L1, 1b: L = L2), with different O2S2 macrocycle systems (L1 and L2) have led to the isolation of the following bis(O2S2 macrocycle) palladium(II) complexes in the solid state: [Pd(L1)2](ClO4)2 (2a) and a mixture of [Pd(L1)2](ClO4)2 (2a) + [Pd(L2)2](ClO4)2 (2b). 相似文献
7.
Rojalin Sahu 《Inorganica chimica acta》2010,363(7):1448-63
In air, hydrated ethanolic (95%) solution of 2-(aminomethyl) substituted pyridine and quinoline, on stirring with half equivalent of Cu(OAc)2·H2O, respectively afforded [Cu(bpca)(OAc)(H2O)]·H2O (1) and [Cu(bqca)(OAc)(H2O)] (2) {bpca = bis(2-pyridylcarbonyl)diimide ion and bqca = bis(2-quinolylcarbonyl)diimide ion} in good yields. These reactions involve oxidation of the methylene group and formation of the bond between nitrogen and carbon in N-C(O) through coupling. The complex [Cu(pqca)(OAc)(H2O)]3[Cu2(OAc)4(EtOH)2]1.5 (3) {pqca = (2-pyridylcarbonyl)(2-quinolylcarbonyl)diimide ion} was synthesized by stirring an ethanolic solution of the Schiff base [(2-pyridyl)-N-((2-quinolyl)methylene)methanamine] (L1) and with one equivalent of Cu(OAc)2·H2O. A plausible mechanism for the conversion has been proposed. The free ligands were isolated as crystalline solids from compounds 1-3, by extrusion of Cu2+ ion using EDTA2−. The molecular structures of 1-3 and bqcaH were established by X-ray crystallography and compounds having quinolyl group have π-stacking interactions. 相似文献
8.
Garima Singh Ajai K. Singh John E. Drake M.B. Hursthouse 《Inorganica chimica acta》2005,358(4):912-918
Two tellurium ligands 1-(4-methoxyphenyltelluro)-2-[3-(6-methyl-2-pyridyl)propoxy]ethane (L1) and 1-ethylthio-2-[2-thienyltelluro]ethane (L2) have been synthesized by reacting nucleophiles [4-MeO-C6H4Te−] and [C4H3S-2-Te−] with 2-[3-(6-methyl-2-pyridyl)propoxy]ethylchloride and chloroethyl ethyl sulfide, respectively. Both the ligands react with HgBr2 resulting in complexes of stoichiometry [HgBr2 · L1/L2] (1/4), which show characteristic NMR (1H and 13C{1H}). On crystallization of 1 from acetone-hexane (2:1) mixture, the cleavage of L1 occurs resulting in 4-MeOC6H4HgBr (2) and [RTe+→HgBr2]Br− (3) (where R = -CH2CH2OCH2CH2CH2-(2-(6-CH3-C5H3N))). The 2 is characterized by X-ray diffraction on its single crystal. It is a linear molecule and is the first such system which is fully characterized structurally. The Hg-C and Hg-Br bond lengths are 2.085(6) and2.4700(7) Å. The distance of four bromine atoms (3.4041(7)-3.546(7) Å) around Hg (cis to C) is greater than the sum of van der Waal’s radii 3.30 Å. This mercury promoted cleavage is observed for an acyclic ligand of RArTe type for the first time and is unique, as there appears to be no strong intramolecular interaction to stabilize the cleavage products. The 4 on crystallization shows the cleavage of organotellurium ligand L2 and formation of a unique complex [(EtS(CH2)2SEt)HgBr(μ-Br)Hg(Br)(μ-Br)2Hg(Br)(μ-Br)BrHg(EtS(CH2)2SEt)] · 2HgBr2 (5), which has been characterized by single crystal structure determination and 1H and 13C{1H} NMR spectra. The elemental tellurium and [C4H3SCH2]2 are the other products of dissociation as identified by NMR (proton and carbon-13). The cleavage appears to be without any transmetalation and probably first of its kind. The centrosymmetric structure of 5 is unique as it has [HgBr3]− unit, one Hg in distorted tetrahedral geometry and one in pseudo-trigonal bipyramidal one. The molecule of 5 may also be described as having [(EtSCH2CH2SEt)HgBr]+ [HgBr3]− units, which dimerize and co-crystallize with two HgBr2 moieties. There are very weak Hg?Br interactions between co-crystallized HgBr2 units and rest of the molecule. [Hg(3)-Br(1)/Hg(3)-Br(4) = 3.148(1)/3.216(1) Å]. The bridging Hg?Br distances, Hg(2)-Br(4)′, Hg(2)′-Br(4) and Hg(1)-Br(2), are from 2.914(1) to 3.008(1) Å. 相似文献
9.
Reactions of labile [MCl3(PPh3)2(NCMe)] (M = Tc, Re) precursors with 1H-benzoimidazole-2-thiol (H2L1), 5-methyl-1H-benzoimidazole-2-thiol (H2L2) and 1H-imidazole-2-thiol (H2L3), in the presence of PPh3 and [AsPh4]Cl gave a new series of trigonal bipyramidal M(III) complexes [AsPh4]{[M(PPh3)Cl(H2L1-3)3]Cl3} (M = Re, 1-3; M = Tc, 4-6). The molecular structures of 1 and 3 were determined by X-ray diffraction. When the reactions were carried out with benzothiazole-2-thiol (HL4) and benzoxazole-2-thiol (HL5), neutral paramagnetic monosubstituted M(III) complexes [M(PPh3)2Cl2(L4,5)] (M = Re, 8, 9; M = Tc, 10, 11) were obtained. In these compounds, the central metal ions adopt an octahedral coordination geometry as authenticated by single crystal X-ray diffraction analysis of 8 and 11. Rhenium and technetium complexes 1, 4 and rhenium chelate compounds 8, 9 have been also synthesized by reduction of [MO4]− with PPh3 and HCl in the presence of the appropriate ligand. All the complexes were characterized by elemental analyses, FTIR and NMR spectroscopy. 相似文献
10.
Tale RH Rodge AH Hatnapure GD Keche AP 《Bioorganic & medicinal chemistry letters》2011,21(15):4648-4651
A series of novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of biological interest were prepared by sequential Bigineli’s reaction, reduction followed by reaction of resulting amines with different arylisocynates. All the synthesized (1-23) compounds were screened against the pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological activity evaluation study reveled that among all the compounds screened, compounds 12 and 17 found to have promising anti-inflammatory activity (68-62% TNF-α and 92-86% IL-6 inhibitory activity at 10 μM). Interestingly compounds 3, 4, 5, 6, 15, 22 and 23 revealed promising antimicrobial activity at MIC of 10-30 μg/mL against selected pathogenic bacteria and fungi. 相似文献
11.
Razia Sultana Renu Sharma Takashiro Akitsu Yoshikazu Aritake 《Inorganica chimica acta》2010,363(13):3432-3441
Heterocyclic thioamides, namely, imidazolidine-2-thione (imdzSH), 1-methyl-1, 3-imidazoline-2-thione (mimzSH), thiazolidine-2-thione (tzdSH) and 2,4-dithiouracil (dtucH2) with silver(I)/copper(I) salts in presence of triphenyl phosphine (PPh3) have yielded complexes of different nuclearity: mononuclear, [Ag(η1-S-HL)(PPh3)2Cl] (HL = imdzSH 1, mimzSH 2, tzdSH 3), dinuclear, [Ag2(η1-S-tzdSH)2(μ-S-tzdSH)2(PPh3)2](NO3)24, and polynuclear, {Cu(μ-S,S-dtucH2)(PPh3)2X} (X = Cl 5, Br 6, I 7). All complexes have been characterized using analytical data, IR and multinuclear NMR spectroscopy (1H, 13C and 31P) and single crystal X-ray crystallography. The thio-ligands are bonded to the metal centers as neutral sulfur donors. The geometry around each metal center is distorted tetrahedral. Complexes 5-7 represent first examples of polymers of 2,4-dithiouracil in its coordination chemistry with metal salts. The hydrogen bonding interactions lead to the formation of 1D (2, 3, 7) and 2D (1, 4-6) sheet structures. 相似文献
12.
Packiarajan M Coate H Desai M Jimenez HN Reinhard EJ Jubian VJ Marzabadi MR Chandrasena G Wolinski TC Walker MW Andersen K 《Bioorganic & medicinal chemistry letters》2011,21(21):6500-6504
Synthesis, SAR and physico-chemical properties of an alkyl aminothiazole series 8 and 16 are described. 2-Pyridylaminothiazole based compounds such as 8c and 16a exhibit high affinity at the NPY5 receptor with desirable c Log Ps and solubilities. However, they also suffer from high in vitro and in vivo clearance. Compound 16a partially inhibits the feeding behavior elicited by i.c.v. injection of the selective NPY5 agonist [cPP1-7, NPY19-23, Ala31, Aib32, Gln34]-human pancreatic polypeptide polypeptide (cPP). 相似文献
13.
Schiff bases of 2-hydroxybenzophenone (HBP) (C6H5)(2-HOC6H4)CN(CH2)nEAr (L1/L2: E = S, Ar = Ph, n = 2/3; L3/L4: E = Se, Ar = Ph, n = 2/3; L5/L6: E = Te, Ar = 4-MeOC6H4, n = 2/3) and their complexes [PdCl(L-H)] (L = L1−L6; 1, 2, 3, 5, 7, 11), [PtCl(L3-H/L5-H)] (4/8), [PtCl2(L4/L6)2] (6/12), [(p-cymene)RuCl(L5/L6)]Cl (9/13) and [HgBr2(L5/L6)2] (10/14) have been synthesized and characterized by proton, carbon-13, selenium-77 and tellurium-125 NMR, IR and mass spectra. Single crystal structures of L1, 1, 3, 4, 5 and 7 were solved. The Pd-E bond distances (Å): 2.2563(6) (E = S), 2.3575(6)−2.392(2) (E = Se); 2.5117(5)−2.5198(5) (E = Te) are near the lower end of the bond length range known for them. The Pt-Se bond length, 2.3470(8) Å, is also closer to the short values reported so far. The Heck and Suzuki reaction were carried out using complexes 1, 3, 5 and 7 as catalysts under aerobic condition. The percentage yields for trans product in Heck reaction were found upto 85%. 相似文献
14.
The dinuclear bis(6-X-pyridin-2-olato) ruthenium complexes [Ru2(μ-XpyO)2(CO)4(PPh3)2] (X = Cl (4B) and Br (5B)), [Ru2(μ-XpyO)2(CO)4(CH3CN)2] (X = Cl (6B), Br (7B) and F (8B)) and [Ru2(μ-ClpyO)2(CO)4(PhCN)2] (9B) were prepared from the corresponding tetranuclear coordination dimers [Ru2(μ-XpyO)2(CO)4]2 (1: X = Cl; 2: X = Br) and [Ru2(μ-FpyO)2(CO)6]2 (3) by treatment with an excess of triphenylphosphane, acetonitrile and benzonitrile, respectively. In the solid state, complexes 4B-9B all have a head-to-tail arrangement of the two pyridonate ligands, as evidenced by X-ray crystal structure analyses of 4B, 6B and 9B, in contrast to the head-to-head arrangement in the precursors 1-3. A temperature- and solvent-dependent equilibrium between the yellow head-to-tail complexes and the red head-to-head complexes 4A-7A and 9A, bearing an axial ligand only at the O,O-substituted ruthenium atom, exists in solution and was studied by NMR spectroscopy. Full 1H and 13C NMR assignments were made in each case. Treatment of 1 and 2 with the N-heterocyclic carbene (NHC) 1-butyl-3-methylimidazolin-2-ylidene provided the complexes [Ru2(μ-XpyO)2(CO)4(NHC)], X = Cl (11A) or Br (12A). An XRD analysis revealed the head-to-head arrangement of the pyridonate ligands and axial coordination of the carbene ligand at the O,O-substituted ruthenium atom. The conversion of 11A and 12A into the corresponding head-to-tail complexes was not possible. 相似文献
15.
A series of osmium(VI) nitrido complexes containing pyridine-carboxylato ligands OsVI(N)(L)2X (L = pyridine-2carboxylate (1), 2-quinaldinate (2) and X = Cl (a), Br (1b and 2c) or CH3O (2b)) and [OsVI(N)(L)X3]− (L = pyridine-2,6-dicarboxylate (3) and X = Cl (a) or Br (b)) have been synthesised. Complexes 1 and 2 are electrophilic and react readily with various nucleophiles such as phosphine, sulfide and azide. Reaction of OsVI(N)(L)2X (1 and 2) with triphenylphosphine produces the osmium(IV) phosphiniminato complexes OsVI(NPPh3)(L)2X (4 and 5). The kinetics of nitrogen atom transfer from the complexes OsVI(N)(L)2Br (2c) (L = 2-quinaldinate) with triphenylphosphine have been studied in CH3CN at 25.0 °C by stopped-flow spectrophotometric method. The following rate law is obtained: −d[Os(VI)]/dt = k2[Os(VI)][PPh3]. OsVI(N)(L)2Cl (L = 2-quinaldinate) (2a) reacts also with [PPN](N3) to give an osmium(III) dichloro complex, trans-[PPN][OsIII(L)2Cl2] (6). Reaction of OsVI(N)(L)2Cl (L = 2-quinaldinate) (2a) with lithium sulfide produces an osmium(II) thionitrosyl complex OsII(NS)(L)2Cl (7). These complexes have been structurally characterised by X-ray crystallography. 相似文献
16.
Lv K Wang LL Liu ML Zhou XB Fan SY Liu HY Zheng ZB Li S 《Bioorganic & medicinal chemistry letters》2011,21(10):3062-3065
We report herein the design and synthesis of novel 1-[3-(dimethylamino)propyl]indolin-2-one derivatives based on the structural features of Sunitinib, a known multitargeted receptor tyrosine kinase inhibitor, and TMP-20, a previously discovered compound with good antitumor activity in our lab. These newly synthesized derivatives were evaluated for in vitro activity against five human cancer cell lines and VEGF/bFGF-stimulated HUVECs. Results revealed that all of the target compounds 1a-p show potent antitumor activity, compounds 1e-h (IC50’s: 0.45-5.08 μM) are more active than Sunitinib (IC50’s: 1.35-6.61 μM), and the most active compound 1h (IC50: 0.47-3.11 μM) is 2.1-4.6-fold more potent than Sunitinib against all five cancer cell lines. In addition, like Sunitinib, 1a-p have higher selectivity on VEGF-stimulated HUVEC other than bFGF-stimulated HUVEC. 相似文献
17.
Mairéad E. Kelly Ralph Kluge Dirk Steinborn Harry Schmidt 《Inorganica chimica acta》2009,362(4):1323-4211
A number of complexes of the types [PtBr2Me2(N?N)] (N?N = 4,4′-di-Me-2,2′-bpy (1); 4,4′-di-t-Bu-2,2′-bpy (2); 2,2′-bpz (3); bpym (4)) and [PtBr2Me2(L)2] (L = H-pz (5); 4-Me-H-pz (6); H-idz (7); H-im (8); H-bim (9); quaz (10)) are reported. Characterization by NMR (1H, 13C and 195Pt), IR and EI-MS is given. In addition, crystal structures of several of these complexes are described. Furthermore, interactions within these structures including intramolecular hydrogen bonding and π-π stacking interactions are reported. The reactivity of selected mononuclear complexes was investigated and yielded two dinuclear complexes [PPh4][(PtBrMe2)2(μ-Br)(μ-pz)2] (11) and [(PtBr2Me2)2(μ-bpym)] (12), respectively. The latter complex is accompanied by a solid-state structure. Finally, the thermal stability of all complexes is reported. 相似文献
18.
do Nascimento FB Von Poelhsitz G Pavan FR Sato DN Leite CQ Selistre-de-Araújo HS Ellena J Castellano EE Deflon VM Batista AA 《Journal of inorganic biochemistry》2008,102(9):1783-1789
The reaction of cis-[RuCl2(dppb)(N-N)], dppb = 1,4-bis(diphenylphosphino)butane, complexes with the ligand HSpymMe2, 4,6-dimethyl-2-mercaptopyrimidine, yielded the cationic complexes [Ru(SpymMe2)(dppb)(N-N)]PF6, N-N = bipy (1) and Me-bipy (2), bipy = 2,2′-bipyridine and Me-bipy = 4,4′-dimethyl-2,2′-bipyridine, which were characterized by spectroscopic and electrochemical techniques and X-ray crystallography and elemental analysis. Additionally, preliminary in vitro tests for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27264 and antitumor activity against the MDA-MB-231 human breast tumor cell line were carried out on the new complexes and also on the precursors cis-[RuCl2(dppb)(N-N)], N-N = bipy (3) and Me-bipy (4) and the free ligands dppb, bipy, Me-bipy and SpymMe2. The minimal inhibitory concentration (MIC) of compounds needed to kill 90% of mycobacterial cells and the IC50 values for the antitumor activity were determined. Compounds 1-4 exhibited good in vitro activity against M. tuberculosis, with MIC values ranging between 0.78 and 6.25 μg/mL, compared to the free ligands (MIC of 25 to >50 μg/mL) and the drugs used to treat tuberculosis. Complexes 1 and 2 also showed promising antitumor activity, with IC50 values of 0.46 ± 0.02 and 0.43 ± 0.08 μM, respectively, against MDA-MB-231 breast tumor cells. 相似文献
19.
Franz A. Mautner Jörg H. Albering Febee R. Louka Salah S. Massoud 《Inorganica chimica acta》2011,365(1):290-296
Three mono-nuclear copper(II) complexes [Cu(tepza)X]ClO4 (X = Cl, 1; X = NCS, 2; X = dca, 3) and two dinuclear bridging complexes [Cu2(tepza)2(μ-C4O4)](ClO4)2·H2O(4) and [Cu2(tepza)2(μ-C5O5)](ClO4)2(5) where tepza = tris[2-ethyl(1-pyrazolyl)]amine, dca = dicyanamide, C4O42− = 3,4-dihydroxycyclobut-3-ene-1,2-dionate (squarate dianion) and C5O52− = 4,5-dihydroxycyclopent-4-ene-1,2,3-trionate (croconate dianion) were synthesized and structurally characterized by IR and UV-Vis spectroscopy as well as by single X-ray crystallography. In the solid state, the geometry of copper(II) centers in these complexes are as follows: close to SP in 2, distorted TBP in 3, predominant SP in 4, and distorted octahedral in 5, whereas in solution distorted SP geometry was generally found. The squarato and the croconato dianions in complexes 4 and 5 are bridging the two copper(II) centers in cis-bis-monodentate and bis-bidentate bonding modes, respectively. Magnetic susceptibility measurements at variable temperatures (2-300 K) reveal the weak antiferromagnetic coupling in the two bridging dinuclear complexes 4 (J = −24.9 cm−1) and 5 (J = −3.1 cm−1). 相似文献
20.
Olivier Schott Abdeslem Bentama Salah-Eddine Stiriba Jorge Pasán Marius Andruh Miguel Julve 《Inorganica chimica acta》2011,376(1):358-366
The preparation, crystal structure and variable temperature-magnetic investigation of three 2-(2′-pyridyl)imidazole-containing chromium(III) complexes of formula PPh4[Cr(pyim)(C2O4)2]·H2O (1), AsPh4[Cr(pyim)(C2O4)2]·H2O (2) and [Cr2(pyim)2(C2O4)2(OH2)2]·2pyim · 6H2O (3) [pyim = 2-(2′-pyridyl)imidazole, , and ] are reported herein. The isomorphous compounds are made up of discrete [Cr(pyim)(C2O4)2]− anions, cations [X = P (1) and As (2)] and uncoordinated water molecules. The chromium environment in 1 and 2 is distorted octahedral with Cr-N and Cr-O bond distances varying in the ranges 2.040(3)-2.101(3) and 1.941(3)-1.959(3) Å, respectively. The angle subtended by the chromium(III) ion by the two didentate oxalate ligands cover the range 82.49(12)-82.95(12)°, values which are somewhat greater than those concerning the chelating pyim molecule [77.94(13) (1) and 78.50(13)° (2)]. Complex 3 contains discrete centrosymmetric [Cr2(pyim)2(C2O4)2(OH)2] neutral units where the two chromium(III) ions are joined by a di-μ-hydroxo bridge, the oxalate and pyim groups acting as peripheral didentate ligands. Uncoordinated water and pyim molecules are also present in 3 and they contribute to the stabilization of its structure by extensive hydrogen bonding and π-π type interactions. The values of the intramolecular chromium-chromium separation and angle at the hydroxo bridge in 3 are 2.9908(12) Å and 99.60(16)°, respectively. Magnetic susceptibility measurements of 1-3 in the temperature range 1.9-300 K show the occurrence of weak inter- (1 and 2) and intramolecular (3) antiferromagnetic couplings. The magnetic properties of 3 have been interpreted in terms of a temperature-dependent exchange integral, small changes of the angle at the hydroxo bridge upon cooling being most likely responsible for this peculiar magnetic behavior. 相似文献