Synthesis, Structure and Antitumour Properties of a New 1,2-Propylenediaminetetraacetate-Ruthenium(III) Compound

A novel complex formed by ruthenium (III) and the sequestering ligand 1,2-propylenediaminetetraacetic acid (PDTA) has been synthetized and characterized. The structure of the monomeric compound, studied by X-ray diffraction , shows an almost symmetric octahedral geometry around the metal ion, with two chlorine atoms in a cis conformation. The antitumour activity against a variety of murine and human cancers is reported.     

Construction of Ru(II) Polypyridyl Based Macrocycles: Synthesis, Characterization, Electrochemical, Li Binding, Antitumour and Anti-HIV properties

Some ruthenium (II) polypyridyl complexes with a bis-chalcone (obtained by the condensation of 3-methyl-thiophene-2-carboxaldehyde and 4-acetyl pyridine) have been synthesized and characterized spectroscopically (IR, NMR, UV/Vis), conductimetric, elemental analysis and FAB mass data. Their luminescent, redox and Li(+) binding properties have been studied. The anti-HIV and antitumour activities have also been reported.     

Platinum(II)-Acyclovir Complexes: Synthesis, Antiviral and Antitumour Activity

A platinum(II) complex with the antiviral drug acyclovir was synthesized and its antiviral and anticancer properties were investigated in comparison to those of acyclovir and cisplatin. The platinum-acyclovir complex maintained the antiviral activity of the parent drug acyclovir, though showing a minor efficacy on a molar basis (ID(50) = 7.85 and 1.02 muMu for platinum-acyclovir and cisplatin, respectively). As anticancer agent, the platinum-acyclovir complex was markedly less potent than cisplatin on a mole-equivalent basis, but it was as effective as cisplatin when equitoxic dosages were administered in vivo to P388 leukaemia-bearing mice (%T/C = 209 and 211 for platinum-acyclovir and cisplatin, respectively). The platinum-acyclovir complex was also active against a cisplatin-resistant subline of the P388 leukaemia (%T/C = 140), thus suggesting a different mechanism of action. The DNA interaction properties (sequence specificity and interstrand cross-linking ability) of platinum-acyclovir were also investigated in comparison to those of cisplatin and [Pt(dien)Cl](+), an antitumour-inactive platinum-triamine compound. The results of this study point to a potential new drug endowed, at the same time, with antiviral and anticancer activity and characterized by DNA interaction properties different from those of cisplatin.     

Synthesis, Characterization and Antitumour Activity of Some Butyltin(IV) Cysteaminates and N,N-Dimethylcysteaminates

The synthesis and characterization of four di- and tri-n-butyltin cysteaminates and N,N-dimethylcysteaminates and three protonated / quaternized derivatives are reported. They all exhibit moderate or high in vitro cytotoxic activity. Six of seven compounds presented in this work are more active than cisplatin, etoposide and 5-fluorouracil, but less active than methotrexate and doxorubicin.     

Synthesis, Characterization and In vitro Antitumour Activity of Novel Organotin Derivatives of 1,2- and 1,7-Dicarba-Closo-dodecaboranes

Several organotin derivatives of 1,2- and 1,7-dicarba-closo-dodecaboranes were synthesized and characterized by ¹¹⁹Sn Mössbauer, ¹H, ¹³C and ¹¹⁹Sn NMR spectroscopy. Their antitumour activities in vitro against cancerous cell lines of human origin are reported.     

Antitumour and Immunomodulatory Effects of Cu(II) Complexes of Thiobenzyhdrazide

Thiiobenzyhdrazide (Htbh) and its Cu(II) complexes, [Cu(Htbh)2Cl2] and [Cu(tbh)2] were synthesized and characterized by various physicochemical studies. In vivo and in vitro antitumour activity of Htbh, [Cu(Htbh)2Cl2] and [Cu(tbh)2] has been tested. LD50 values were calculated for all the three compounds. It was observed that the antitumour effect of [Cu(Htbh)2Cl2] is maximum. Light microscopic study of the treated tumour mass demonstrated that certain cellular degradation, such as disappearance of mitotic figures, loss in cellular compactness, distortion of nucleus and disruption of cytoplasmic boundaries, takes place in the tumour region of complex treated mice. Further, tumour bearing mice administered with Cu(II) complexes showed reversal of tumour growth associated induction of apoptosis in lymphocytes.     

Copper(II) Mediated Homo-Coupling of 1,2-difluorovinylstannanes

The reaction of substituted 1,2-difluorovinylstannanes with anhydrous Cu(OAc)₂ in dimethylformamide, under an oxygen atmosphere, at room temperature stereospecifically gives the corresponding symmetrical 1,3-dienes in good to excellent yields. Moisture drastically reduces the yield of homo-coupled product and produces significant amounts of RCF=CFH. The Cu(II) promoted homo-coupling of the fluorinated vinylstannanes is superior to the Cu(I)Cl mediated homo-coupling of the corresponding hydrocarbon vinylstannanes. When 1,2-difluorovinylstannanes are treated with Cu(I)Cl, the reaction is sluggish and significant amounts of RCF=CFH are formed.     

Synthesis, Characterization and Biological Evaluation of Co(II), Cu(II), Ni(II) and Zn(II) Complexes With Cephradine

Some Co(II), Cu(II), Ni(II) and Zn(II) complexes of antibacterial drug cephradine have been prepared and characterized by their physical, spectral and analytical data. Cephradine acts as bidentate and the complexes have compositions, [M(L)(2)X(2)] where [M = Co(II), Ni(II) and Zn(II), L = cephradine and X = Cl(2)] showing octahedral geometry, and [M(L)(2)] where [M = Cu(II), L = cephradine] showing square planar geometry. In order to evaluate the effect of metal ions upon chelation, eephradine and its complexes have been screened for their antibacterial activity against bacterial strains, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.     

Synthesis, Characterization and Antiproliferative Activity of the Co(II), Ni(II), Cu(II), Pd(II) and Pt(II) Complexes of 2-(4-Thiazolyl)Benzimidazole (Thiabendazole)

Complexes of 2-(4-thiazolyi)benzimidazole (thiabendazole, THBD) with Co(II), Ni(II), Cu(ll) of general formula ML(2)(NO(3))(2) H(2)O and complexes of Pd(II) and Pt(II) of general formula ML2Cl(2) H(2)O have been obtained and characterized by elemental analyses, IR and far IR spectroscopy and magnetic measurements. The X-ray crystal structure of the copper(II) complex has been determined. The in vitro cell proliferation inhibitory activity of these compounds was examined against human cancer cell lines A 549 (lung carcinoma), HCV-29 T (urinary bladder carcinoma), MCF-7 (breast cancer), T47D (breast cancer), MES-SA (uterine carcinoma) and HL-60 (promyelocytic leukemia). Pt-THBD has been found to exhibit an antileukemic activity of the HL-60 line cells matching that of an arbitrary criterion.     

Formation, Characterization and Electrical Conductivity of Polycarbosilazane-Cu(II), -Ni(II) and -Cr(III) Chloride Metallopolymers

A series of transition metal-polycarbosilazane complexes have been prepared by the reaction of poly(N,N-bis(dimethylsilyl)ethylenediamine), [–Si(CH₃)₂NHCH₂CH₂NH–] _n , with Cu(II), Ni(II), and Cr(III) chloride. The resulting complexes were characterized by infrared (FT-IR) and UV-visible spectroscopy, magnetic susceptibility measurements, thermogravimetric analysis (TGA), and powder X-ray diffraction (XRD). The average chain-chain spacing in these materials were estimated from XRD data and found to be 6.88, 7.91, 7.09, and 6.33 Å in metal-free, Cu(II)-, Ni(II)-, and Cr(III)-containing polycarbosilazanes, respectively. DC electrical conductivity measurements showed that all these metal-polycarbosilazane complexes exhibit semiconductor behavior while the metal-free matrix is an insulator.     

Synthesis of (N,N'-Bis(2-Hydroxyethyl)Ethane-1,2-Diamine)Malonatoplatinum(II) and X-Ray Crystal Structure of the Cis-R,S-Isomer

Hydroxyethyl substituted amineplatinum(II) and (IV) complexes are an interesting class of platinum based antitumour compounds due to their uncoordinated hydroxy groups. These hydroxy groups could play an important role in the mode of action of such complexes with respect to their ability to act as donor or acceptor for hydrogen bonds. Moreover, their chemistry in solution is of interest because it was found that there is the possibility of an intramolecular attack to form ethanolatoamine chelated species which are responsible for very stable monoadducts with 5'-GMP. Furthermore, there is the possibility of derivatisation at the OH site to form a new series of platinum compounds which may be used for a carrier mediated transport to tumour tissues. In this context a series of (N,N'-bis(2-hydroxyethyl)ethane-l,2-diamine)-platinum(II) complexes has been synthesised. During purification of one of the platinum based compounds, it was possible to isolate (SP-4-3)-R,S-(N,N'-bis(2-hydroxyethyl)ethane-l,2-diamine)malonatoplatinum(ll) and to resolve the structure by single crystal structure analysis. Intra- and intermolecular hydrogen bonds have been found which may explain the spontaneous crystallisation of the cis-R,S isomer and the stabilisation of the boat conformation of the malonatoplatinum(II) six-membered ring.     

Toxicity, Spectroscopic Characterization and Electrochemical Behaviour of New Macrocclic Complexes of Lead(II) and Palladium(II) Metals

Tetraazamacrocyclie complexes of lead and palladium have been synthesized by the template process using the bis(benzil)ethylenediamine precursor. The tetradentate macrocycle (maL) reacts with PbCl(2), PdCl(2) and different diamines in a 1:1:1 molar ratio in methanol to give several solid complexes of the types [Pb(maL)(R)Cl(2)] and [Pd(maL)(R)]Cl(2) (where R = 2,6-diaminopyridine or 1,2-phenylenediamine). The macrocycle and its metal complexes have been characterized by elemental analysis, molecular weight determinations, molar conductivity, IR, (1)H NMR, (13)C NMR, electronic, mass and electrochemical studies. The macrocyclic ligand coordinates through the four azomethine nitrogen atoms which are bridged by benzil moieties. IR spectra suggest that the pyridine nitrogen is not coordinating. The palladium complexes exhibit tetracoordinated square-planar geometry, whereas a hexacoordinated octahedral geometry is suggested for lead complexes. The macrocycle along with its complexes have been screened in vitro against a number of pathogenic fungi and bacteria to assess their growth inhibiting potential.     

Synthesis,crystal structures and spectral characterization of trans-bisaquabis(o-vanillinato)copper(II), cis-aquabis(o-vanillinato)copper(II) and aqua[bis(o-vanillinato)-1,2-ethylenediimin]copper(II)

trans-Bisaquabis(o-vanillinato)copper(II) (I), cis-aquabis(o-vanillinato)copper(II) (II) and aqua[bis(o-vanillinato)-1,2-ethylenediimin]copper(II) (III) complexes were synthesized and characterized by means of elemental analysis, IR and UV–vis spectroscopy, thermal analysis and X-ray diffraction techniques. The coordination geometry around Cu(II) is a octahedral with coordination number of six for I and is a square-pyramidal with coordination number of five for both II and III. In all three compounds, a three-dimensional structure is formed via C–H⋯O hydrogen-bond interactions and intermolecular π–π and π-ring interactions. The compounds I and III have two-dimensional hydrogen-bonded step-chain structure in xz-plane, while compound II has a zigzag chain structure in xy-plane. On the basis of the first DTA_max of the anhydrous complexes of I and II, the thermal stability sequence is trans-isomer > cis-isomer. This fact should be related with the binding of the ligand.     

Synthesis,Characterization and Catalytic Activities of Palladium(II) Nitroaryl Complexes

Two palladium(II) nitroaryl complexes trans-[bromo(p-nitrophenyl)bis(triphenylphosphine)palladium(II)] 1 and trans-[bromo(2,4-dinitrophenyl)bis(triphenylphosphine)palladium(II)] 2 have been synthesized. The complexes were characterized by FTIR and NMR (¹H, ¹³C and ³¹P) spectroscopy and elemental analysis. The molecular structure of complex 2, as confirmed by X-ray crystallography, reveals that the Pd atom and its neighboring groups (two PPh₃, Br and phenylene group) lie in a slightly distorted square plane. In the UV–Vis spectra of the complexes 1 and 2, the palladium to aryl charge transfer bands were observed. The emission peaks from the singlet excited states (S₁ → S₀) were observed in the photoluminescence spectra of the complexes. The thermal stability of the complexes has been studied by thermal gravimetric analysis (TGA). TGA data showed that both complexes are thermally stable up to 200 °C, and complex 1 is more stable than 2. The catalytic efficiency of the new palladium(II) complexes was studied as demonstrated using the Sonogashira coupling reactions with good yields. The experimental results suggest that the Sonogashira coupling reactions can be performed at moderate temperature (50 °C) using these new palladium(II) complexes as catalysts.     

二二甲亚砜合硫氰酸镉（DSTC）晶体的合成、结构、表征与晶体生长

合成了金属有机配合物晶体二二甲亚砜合硫氰酸镉Cd(SCN) 2 (C2 H6 OS) 2 (简称DSTC)。用X射线四圆衍射方法确定了此化合物的晶体结构。用元素分析、红外光谱对其进行了化学表征。首次在DMSO/水的溶剂中 ,生长出尺寸为 3 5mm× 12mm× 11mm透明单晶。     

Di-n-Butyl-, Tri-n-Butyl- and Triphenyltin dl-Terebates: Synthesis, Characterization and In Vitro Antitumour Activity

Di-n-butyltin, tri-n-butyltin and triphenyltin terebates were screened against several human tumour cell lines and found comparably or more active than carboplatin, cis-platin, 5-fluorouracil, methotrexate and doxorubicin, some reference compounds used clinically.     

Synthesis and Characterization of Coordinatively Unsaturated Copper (II) Complexes of 1,3-Bis(2'-Pyridyl)-1,2-Diaza-2-Butene and Their Antityrosinase Activity

The coordinatively unsaturated copper (II) complexes of 1,3-bis(2'-pyridyl)-1,2-diaza-2- butene with different ancillary anions were synthesized which can bind to copper centers of tyrosinase enzyme. The compounds were found to exhibit inhibitory activities against mushroom tyrosinase and the nature and extent of inhibition is modulated according to the type of ancillary anions.     

硫氰酸锰及其相关衍生物的合成及化学表征

合成了金属有机配合物非线性光学晶体硫氰酸汞锰，及其相关衍生物，二二甲亚砜合硫氰酸汞锰，乙二醇一甲醚合硫氰酸汞锰，二水合二N，N－二甲基乙酰胺合硫氰酸汞锰，二水合二N－甲基－α－吡咯烷酮合硫氰酸汞锰。采用元素分析，红外光谱以及紫外－可见－近红外透央求我谱分析对其进行了化学表征。