http://www.hindawi.comThe latest articles from Hindawi Publishing Corporation© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/276109Photodynamic therapy (PDT) is a treatment modality that has been used in the successful treatment of a number of diseases and disorders, including age-related macular degeneration (AMD), psoriasis, and certain cancers. PDT uses a combination of a selectively localised light-sensitive drug (known as a photosensitiser) and light of an appropriate wavelength. The light-activated form of the drug reacts with molecular oxygen to produce reactive oxygen species (ROS) and radicals; in a biological environment these toxic species can interact with cellular constituents causing biochemical disruption to the cell. If the homeostasis of the cell is altered significantly then the cell enters the process of cell death. The first photosensitiser to gain regulatory approval for clinical PDT was Photofrin. Unfortunately, Photofrin has a number of associated disadvantages, particularly pro-longed patient photosensitivity. To try and overcome these disadvantages second and third generation photosensitisers have been developed and investigated. This Review highlights the key photosensitisers investigated, with particular attention paid to the metallated and non-metallated cyclic tetrapyrrolic derivatives that have been studied in vitro and in vivo; those which have entered clinical trials; and those that are currently in use in the clinic for PDT.Leanne B. Josefsen and Ross W. Boyle© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/286363Jannie C. Swarts, Michael J. Cook, and Edward N. Baker© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/875410New bidentate or tridentate Schiff bases and their VO(II) and Co(II) complexes formed by the condensation of methyl isobutyl ketone with nicotinamide (mna)/2-amino-4-chlorophenol (map) and 2-hydroxy acetophenone with nicotinamide (han)/isoniazide (hai). Physicochemical characterization has been carried out to determine the structure of the complexes. The FAB mass and thermal data show degradation pattern of the complexes. XRD analysis reveals that all the studied complexes crystallize as tetragonal crystal system. Some of the complexes have been screened for their antimicrobial activity by the well diffusion technique using DMSO as solvent on different species of pathogenic bacteria/fungi, that is, E. coli, S. aureus, S. fecalis, A. niger, T. polysporum, and their antimicrobial potency have been discussed. It has been found that all the complexes are antimicrobially active and show higher activity than the free ligand. Metal chelation affects significantly the antimicrobial/bioactive behavior of the organic ligands.A. P. Mishra and Monika Soni© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/716329Medicinal inorganic chemistry has been stimulating largely by the success of the anticancer drug, cisplatin. Various metal complexes are currently used as therapeutic agents (e.g., Pt, Au, and Ru) in the treatment of malignant diseases, including several types of cancers. Understanding the mechanism of action of these metal-based drugs is for the design of more effective drugs. Proteomic approaches combined with other biochemical methods can provide comprehensive understanding of responses that are involved in metal-based anticancer drugs-induced cell death, including insights into cytotoxic effects of metal-based anticancer drugs, correlation of protein alterations to drug targets, and prediction of drug resistance and toxicity. This information, when coupled with clinical data, can provide rational basses for the future design and modification of present used metal-based anticancer drugs.Ying Wang and Jen-Fu Chiu© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/384010A class of Ag(I) N-heterocyclic carbene silver complexes, 1–3, derived from 4,5-dichloro-1H-imidazole has been evaluated for their anticancer activity against the human cancer cell lines OVCAR-3 (ovarian), MB157 (breast), and Hela (cervical). Silver complexes 1–3 are active against the ovarian and breast cancer cell lines. A preliminary in vivo study shows 1 to be active against ovarian cancer in mice. The results obtained in these studies warrant further investigation of these compounds in vivo.Doug A. Medvetz, Khadijah M. Hindi, Matthew J. Panzner, Andrew J. Ditto, Yang H. Yun, and Wiley J. Youngs© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/469531Cancerous diseases present a formidable health problem worldwide. While the chemotherapy of cancer, in conjunction with other treatment modalities, has reached a significant level of maturity, efficacious use of such agents is still restricted by numerous pharmacological deficiencies, such as poor water solubility, short serum circulation lifetimes, and low bioavailability resulting from lack of affinity to cancer tissue and inadequate mechanisms of cell entry. More critically still, most drugs suffer from toxic side effects and a risk of drug resistance. The class of platinum anticancer drugs, although outstandingly potent, is particularly notorious in that respect. Among the countless methods developed in recent years in an effort to overcome these deficiencies, the technology of polymer-drug conjugation stands out as a particularly advanced treatment modality. The strategy involves the bioreversible binding, conjugating, of a medicinal agent to a water-soluble macromolecular carrier. Following pharmacokinetic pathways distinctly different from those of the common, nonpolymeric drugs, the conjugate so obtained will act as a prodrug providing safe transport of the bioactive agent to and into the affected, that is, cancerous cell for its ultimate cell-killing activity. The present treatise will acquaint us with the pharmacological fundamentals of this drug delivery approach, applied here specifically to the metalorganic platinum-type drug systems and the organometallic ferrocene drug model. We will see just how this technology leads to conjugates distinctly superior in antiproliferative activity to cisplatin, a clinically used antitumor agent used here as a standard. Polymer-drug conjugation involving metal-based and other medicinal agents has unquestionably matured to a practical tool to the pharmaceutical scientist, and all indications point to an illustrious career for this nascent drug delivery approach in the fight against cancer and other human maladies.Eberhard W. Neuse© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/745989A kinetic study of the aqua substitution in the [TcO(OH2)(CN)4]− complex by different thiourea ligands (TU = thiourea, NMTU = N-methyl thiourea, NNDMTU = N, N′-dimethylthiourea) yielded second-order formation rate constants (25∘C) as follows [NNDMTU, NMTU, TU, respectively]: kf = 11.5 ± 0.1, 11.38 ± 0.04, and 7.4 ± 0.1 M−1s−1, with activation parameters: ΔHkf#:55±2, 42±3, 35±5 kJ mol−1; ΔSkf#:−40±8, −84±11, −110±17 J K−1mol−1. A subsequent high-pressure investigation of the aqua substitution in the [ReO(OH2)(CN)4]− and [TcO(OH2)(CN4)]− complexes by selected entering ligands yielded ΔVkf# values as follows: Re(V): −1.7±0.3(NCS−), −22.1±0.9 (TU) and for Tc(V): −3.5±0.3(NCS−), −14±1 (NNDMTU), and−6.0±0.5 (TU) cm3mol−1, respectively. These results point to an interchange associative mechanism for the negative NCS− as entering group but even a pure associative mechanism for the neutral thiourea ligands.J. Mattheus Botha and Andreas Roodt© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/260146Arsenic-based compounds have become accepted agents for cancer therapy providing high rates of remission of some cancers such as acute promyelocytic leukemia (APL). The mechanisms by which arsenic-containing compounds kill cells and reasons for selective killing of only certain types of cancer cells such as APLs have recently been delineated. This knowledge was gained in parallel with increasing understanding and awareness of the importance of intracellular redox systems and regulation of the production of reactive oxygen species (ROS) by controlling mitochondrial function. Many of the targets for the arsenic-containing compounds are mitochondrial proteins involved in regulating the production of ROS. Inhibition of these proteins by disulfide linkage of vicinal thiol groups often leads to increased production of ROS and induction of apoptotic signalling pathways. Sensitivity or resistance to the actions of arsenic-containing compounds on cancer cells and normal cells depends on the levels of transport systems for their uptake or efflux from the cells as well as their redox defence mechanisms. The exact mechanisms of arsenic toxicity as well as its anticancer properties are likely to be related and these aspects of arsenic metabolism are covered in this review. Greater understanding of the mechanisms of action of arsenic will help determine the risks of human exposure to this chemical. Novel organic arsenic-containing compounds and the lessons learned from studying their selective sensitivity in targeting dividing endothelial cells to inhibit angiogenesis raise the future possibility for designing better targeted antineoplastic arsenic-containing compounds with less toxicity to normal cells.Stephen John Ralph© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/576104Platinum drugs continue to be major chemotherapy drugs for cancer treatment. Nevertheless, acquired or intrinsic resistance to these compounds is common in human tumors. One important mechanism for this resistance is the avoidance of cells entering the apoptotic pathway. Nuclear factor-kappa B (NF-kappa B, NF-κB) is a pleiotropic transcription factor key in determining the death threshold of human cells. This factor is important in the final response of cells to platinum drugs, as exemplified by in vitro and in vivo models showing that inhibition of NF-κB sensitizes cancer cells to the effects of these drugs. New approaches focusing on the inhibition of NF-κB could help to minimize or even eliminate intrinsic or acquired resistance to platinum drugs.Vilma Maldonado Lagunas and Jorge Meléndez-Zajgla© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/723634Synthesis of two new water-soluble mixed ligand [Pd(bpy)(dahmp)]Cl and [Ag(bpy)(Hdahmp)]NO3 complexes (dahmp and Hdahmp are the deprotonated monoanion and the protonated neutral 4,6-diamino-5-hydroxy-2-mercaptopyrimidine, resp.) is reported. The composition of the reported complexes was discussed on the bases of IR, H1 NMR, and mass spectra, as well as conductivity and thermal measurements. The reported complexes display a significant anticancer activity against Ehrlich ascites tumor cells (EACs). The higher activity of these complexes with their higher conductivity values corresponds to their complete ionization in aqueous solution.Sahar I. Mostafa and Farid A. Badria© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/417897The impressive impact of cisplatin on cancer on one side and severe side effects, as well as the development of drug resistance during treatment on the other side, were the factors motivating scientists to design and synthesize new more potent analogues lacking disadvantages of cisplatin. Platinum(IV) complexes represent one of the perspective groups of platinum-based drugs. In this review, we summarize recent findings on both in vitro and in vivo effects of platinum(IV) complexes with adamantylamine. Based on a literary overview of the mechanisms of activity of platinum-based cytostatics, we discuss opportunities for modulating the effects of novel platinum complexes through interactions with apoptotic signaling pathways and with cellular lipids, including modulations of the mitochondrial cell death pathway, oxidative stress, signaling of death ligands, lipid metabolism/signaling, or intercellular communication. These approaches might significantly enhance the efficacy of both novel and established platinum-based cytostatics.Alois Kozubík, Alena Vaculová, Karel Souček, Jan Vondráček, Jaroslav Turánek, and Jiřina Hofmanová© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/864653In this study we compared the effects of two previously described antimitochondrial gold complexes, that is, [A] [Au(dppe)2]Cl and [B] [Au(d4pype)2]Cl with two novel lipophilic cations, that is, [C] [Au(dpmaaH2)(dpmaaSnMe2)]Cl and [D] [Au(dpmaaSnMe2)2]Cl as antimitochondrial agents. The results of this study indicate that [C] and [D] have intermediate partition coefficients and exhibited a selective uptake by cells. They exhibited a higher selectivity for the various cell lines than [A] but were more cytotoxic than [B]. There is a significant correlation between the cytotoxic potential of [A], [B], [C], and [D] and their octanol/water partition coefficients in both MCF-7 (breast cancer) and MCF-12A (nonmalignant breast) cells, whereas their cytotoxic potential and ability to induce the release of cytochrome c correlated only in the case of the MCF-12A cells. Complexes [C] and [D] are promising new chemotherapeutic drugs. These compounds target the mitochondrial membranes of certain cancer cells exploiting the differences between the mitochondrial membrane potential of these cells and normal cells. Although the concentrations of these compounds necessary to eradicate cancer cells are very high, the results provide a basis for the synthesis of a new family of compounds with intermediate partition coefficients compared to [A] and [B] but with increased activity against cancer cells.Sherika Mahepal, Richard Bowen, Messai Adenew Mamo, Marcus Layh, and Constance Elizabeth Jansen van Rensburg© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2007/16260Gianni Sava© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/498916The synthesis of phosphorous oxide triazatetrabenzcorroles (TBC) tetra- (9, 11) or octa- (13) substituted on the ring with halogenated functional groups is reported. The complexes are not aggregated in dimethylsulfoxide (DMSO) and show solubility in solvents such as pyridine. The Q band absorption spectra of the complexes are red-shifted compared to unsubstituted PTBC. The latter complex shows a large triplet lifetime (1.7 milliseconds), higher than for MPc derivatives. The chlorinated derivatives show good triplet yields (ΦT∼ 0.46 and 0.36) and relatively long lifetimes (256 and 452 microseconds), respectively, for 11 and 13.Edith M. Antunes and Tebello Nyokong© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/392090The phthalocyanine analogue containing nonperipheral long alkyl-substituted benzenoid rings and pyridine rings, zinc bis(1,4-didecylbenzo)-bis(2,3-pyrido) porphyrazine, was synthesized. Zinc bis(1,4-didecylbenzo)-bis(2,3-pyrido) porphyrazine reacted with dimethyl sulfate and monochloroacetic acid to produce their quaternized products and diethyl sulfate to produce the sulfo-substituted products. All quaternized and sulfo-substituted showed amphiphilic character. Identical peaks in cyclic voltammograms appeared for these products before and after quaternization. During the evaluation of zinc bis(1,4-didecylbenzo)-bis(2,3-pyrido) porphyrazine for its photodynamic therapy of cancer (PDT) efficacy by cancer cell culture, the light exposed dimethyl sulfate quaternized zinc bis(1,4-didecylbenzo)-bis(2,3-pyrido) porphyrazines in IU-002 cells produce cell disruption that can be detected as a decrease in fluorescence.Keiichi Sakamoto, Eiko Ohno-Okumura, Taku Kato, Masaki Watanabe, and Michael J. Cook© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2007/12635In medicinal chemistry field, the biochemical pathways, involved in 7-transmembrane domains G-protein coupled receptors (GPCRs) activation, are commonly studied to establish the activity of ligands towards GPCRs. The most studied steps are the measurement of activated GTP-α subunit and stimulated intracellular cAMP. At the present, many researchers defined agonist or antagonist activity of potential GPCRs drugs employing [35S]GTPγS or [3H]cAMP as probes. Recently, the corresponding lanthanide labels Eu-GTP and Eu-cAMP as alternative to radiochemicals have been developed because they are highly sensitive, easy to automate, easily synthesized, they display a much longer shelf-life and they can be used in multilabel experiments. In the present review, the receptor-drug interaction by europium employment for studying the biochemical pathway of GPCR activation has been focused. Moreover, comparative studies between lanthanide label probes and the corresponding radiolabeled compounds have been carried out.Colabufo Nicola Antonio, Perrone Maria Grazia, Contino Marialessandra, Berardi Francesco, and Perrone Roberto© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2007/37348New lanthanide(III) complexes with 2-[2-hydroxy-3-methoxyphenyl]-3-[hydroxyl-3-methoxybenzylamino]-1,2-dihydroquin-azoline-4(3H)-one (Hmpbaq) have been synthesized and characterized by elemental analysis, conductance measurements, magnetic susceptibilities, spectroscopic (IR, NMR, UV, EPR), and thermal studies. Molar conductance studies indicate 1 : 1 electrolytic behavior for these complexes. IR spectra indicate that Hmpbaq acts as a tridentate ligand coordinating through carbonyl oxygen, benzyl amine nitrogen, and deprotonated phenolic oxygen. TG and DTA studies of La(III) and Pr(III) complexes indicate the presence of two coordinated water molecules. Based on these studies, the complexes have been formulated as [La(mpbaq)2(H2O)2]·NO3, where Ln = La(III), Pr(III), Nd(III), Sm(III), Eu(III), Gd(III), Th(III), Dy(III), and Y(III). The ligand, lanthanide(III) salts, and the corresponding complexes have been simultaneously screened for their antibacterial and antifungal activities and compared with the drugs in use.Kalagouda B. Gudasi, Vidyadhar C. Havanur, Siddappa A. Patil, and Basavaraj R. Patil© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/217573The general synthetic strategy towards water-soluble biodegradable drug carriers and the properties that they must have are discussed. The syntheses of water-soluble biodegradable copolymers of lysine and aspartic acid as potential drug-delivering devices, having amine-functionalised side chains are then described. Covalent anchoring of carboxylic acid derivatives of the antineoplastic ferrocene and photodynamically active phthalocyanine moieties to the amine-containing drug carrier copolymers under mild coupling conditions has been achieved utilising the coupling reagent O-benzotriazolyl-N,N,N′,N′-tetramethyluronium hexafluorophosphate to promote formation of the biodegradable amide bond. Even though the parent antineoplastic ferrocene and phthalocyanine derivatives are themselves insoluble in water at pH < 7, the new carrier-drug conjugates that were obtained are well water-soluble.M. David Maree, Eberhard W. Neuse, Elizabeth Erasmus, and Jannie C. Swarts© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/289490Helicobacter pylori (H. pylori) is a widespread human pathogen causing peptic ulcers and chronic gastritis. Maintaining nickel homeostasis is crucial for the establishment of H. pylori infection in humans. We used immobilized-nickel affinity chromatography to isolate Ni-related proteins from H. pylori cell extracts. Two-dimensional gel electrophoresis and mass spectrometry were employed to separate and identify twenty two Ni-interacting proteins in H. pylori. These Ni-interacting proteins can be classified into several general functional categories, including cellular processes (HspA, HspB, TsaA, and NapA), enzymes (Urease, Fumarase, GuaB, Cad, PPase, and DmpI), membrane-associated proteins (OM jhp1427 and HpaA), iron storage protein (Pfr), and hypothetical proteins (HP0271, HP jhp0216, HP jhp0301, HP0721, HP0614, and HP jhp0118). The implication of these proteins in nickel homeostasis is discussed.Xuesong Sun, Ruiguang Ge, Jen-Fu Chiu, Hongzhe Sun, and Qing-Yu He© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/284691Three novel zinc(II) phthalocyanines substituted with one or two 3,4,5-tris(3,6,9-trioxadecoxy)benzoxy group(s) have been prepared and spectroscopically characterized. These compounds are highly soluble and remain nonaggregated in N,N-dimethylformamide. Upon excitation, they exhibit a relatively weak fluorescence emission and high efficiency to generate singlet oxygen compared with the unsubstituted zinc(II) phthalocyanine. These amphiphilic photosensitizers formulated with Cremophor EL are highly photocytotoxic against HT29 human colon adenocarcinoma and HepG2 human hepatocarcinoma cells. The mono-α-substituted analogue 4 is particularly potent with IC50 values as low as 0.02 μM. The higher photodynamic activity of this compound can be attributed to its lower aggregation tendency in the culture media as shown by absorption spectroscopy and higher cellular uptake as suggested by the stronger intracellular fluorescence, resulting in a higher efficiency to generate reactive oxygen species inside the cells.Jian-Yong Liu, Xiong-Jie Jiang, Wing-Ping Fong, and Dennis K. P. Ng© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/281843A molecularly imprinted polymer (MIP) for tri-O-acetyladenosine (TOAA), PPM(TOAA), was prepared by the combined use of methacrylic acid (MAA) and Zn(II)tetra(4'-methacryloxyphenoxy) phthalocyanine as functional monomers. This MIP exhibited a higher binding ability for TOAA compared to the MIP prepared using only MAA, PM(TOAA), in batch rebinding tests. Scatchard analysis gave a higher association constant of PPM(TOAA) for TOAA (2.96×104 M−1) than that of PM(TOAA) (1.48×104 M−1). The MIP prepared using only the zinc-phthalocyanine, PP(TOAA), did not show any binding capacity for TOAA. This means that the phthalocyanine in the MIP contributes to higher affinities, although it barely interacts with TOAA. Since selectivity for this kind of MIPs is more important than binding affinity, the binding of TOAA and a structurally related compound, tri-O-acetyluridine (TOAU), on the polymers was investigated. Both PPM(TOAA) and PM(TOAA) exhibited binding affinities for TOAA while they did not show any binding capacity for TOAU.Luigia Longo and Giuseppe Vasapollo© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/362105The synthesis, structure, electrochemistry, and biological studies of Co(II), Ni(II), Cu(II), and Zn(II) complexes of thiocarbohydrazone ligand are described. The ligand is synthesized starting from thiocarbohydrazide and isatin. It is evident from the IR data that in all the complexes, only one part of the ligand is coordinated to the metal ion resulting mononuclear complexes. The ligand coordinates essentially through the carbonyl oxygen of the isatin fragment, the nitrogen atom of the azomethine group, and sulfur atom after deprotonation to give five membered rings. H1 NMR spectrum of the ligand shows only one set of signals for the aromatic protons, while the NH of isatin and NH of hydrazone give rise to two different singlets in the 11–14 ppm range. The formulations, [Cu(L)Cl]·2H2O, [Cu(L)(CH3COO)]·2H2O, [Ni(L)Cl], [Ni(L)(CH3COO)], [Co(L2)], and [Zn(L2)]·2H2O are in accordance with elemental analyses, physical, and spectroscopic measurements. The complexes are soluble in organic solvents. Molar conductance values in DMF indicate the nonelectrolytic nature of the complexes. Copper complex displays quasireversible cyclic voltametric responses with Ep near −0.659 v and 0.504 v Vs Ag/AgCl at the scan rate of 0.1 V/s. Copper(II) complexes show a single line EPR signals. For the observed magnetic moment and electronic spectral data possible explanation has been discussed. From all the available data, the probable structures for the complexes have been proposed. The compounds synthesized in present study have shown promising cytotoxic activity when screened using the in vitro method and at the same time were shown to have good activity when tested using the Ehrlich ascites carcinoma (EAC) model. The antimicrobial screening showed that the cobalt complex possesses enhanced antimicrobial activity towards fungi.M. P. Sathisha, V. K. Revankar, and K. S. R. Pai© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/495123Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to introduce diversity sites in the side chain of ferroquine in order to develop a series of ferroquine derivatives. The replacement of the ferrocenyl moiety with ruthenocene has given rise to ruthenoquine and a modest series of analogues. The reaction of ferroquine and selected analogues with Au(PPh3)NO3, Au(C6F5)(tht), and [Rh(COD)Cl2] has resulted in a series of heterobimetallic derivatives. In all cases, compounds have been evaluated for in vitro antiplasmodial activity in both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Preliminary structure-activity relationships have been delineated.Margaret A. L. Blackie and Kelly Chibale© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/754358From the carbolithiation of 6-N,N-dimethylamino fulvene (3) and 2,4[bis(N,N-dimethylamino)methyl]-N-methylpyrrolyl lithium (2a), N-(N′,N′-dimethylaminomethyl)benzimidazolyl lithium (2b)' or p-(N,N-dimethylamino)methylphenyl lithium (2c), the corresponding lithium cyclopentadienide intermediate (4a–c) was formed. These three lithiated intermediates underwent a transmetallation reaction with TiCl4' resulting in N,N-dimethylamino-functionalised titanocenes 5a–c. When these titanocenes were tested against a pig kidney epithelial cell line (LLC-PK), the IC50 values obtained were of 23, and 52 μM for titanocenes 5a and 5b, respectively. The most cytotoxic titanocene in this paper, 5c with an IC50 value of 13 μM, was found to be approximately two times less cytotoxic than its analogue Titanocene C (IC50=5.5 μM) and almost four times less cytotoxic than cisplatin, which showed an IC50 value of 3.3 μM when tested on the LLC-PK cell line.Megan Hogan, James Claffey, Eoin Fitzpatrick, Thomas Hickey, Clara Pampillón, and Matthias Tacke© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/391418The porphyrazines (pzs), a class of porphyrin analogues, are being investigated for their potential use as tumor imaging/therapeutic agents. We here examine six peripherally-functionalized M[pz(AnB4-n)] pzs with n=4, 3, or 2 (in a trans conformation) and M = H2 or Zn, where A is an [S((CH2)2O)4Me]2 unit and B is a fused β,β′-diisopropyloxybenzo group. Cell viability/proliferation assays and fluorescence microscopy were carried out in both tumor and normal cells. Dark toxicity studies disclosed that four of the compounds exhibited toxicity in both normal and tumor cells; one was nontoxic in both normal and tumor cells, and one was selectively toxic to normal cells. Additionally, three of the pzs showed enhanced photo-induced toxicity with these effects in some cases being observed at treatment concentrations of up to ten-fold lower than that needed for a response in Photofrin. All six compounds were preferentially absorbed by tumor cells, suggesting that they have potential as in vitro diagnostic agents and as aids in the isolation and purification of aberrant cells from pathological specimens. In particular, two promising diagnostic candidates have been identified as part of this work.Sangwan Lee, Benjamin J. Vesper, Hong Zong, Neal D. Hammer, Kim M. Elseth, Anthony G. M. Barrett, Brian M. Hoffman, and James A. Radosevich© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2008/275084Two novel cobalt(III) pyridine complexes (1)[Co(en)2(py)2]3+ and (2)[Co(en)2(mepy)2]3+ (en=ethylenediamine, py=pyridine, and mepy=methylpyridine) have been synthesized and characterized. The interaction of these complexes with calf thymus DNA was investigated by absorption, emission spectroscopy, viscosity measurements, DNA melting, and DNA photocleavage. Results suggest that the two complexes bind to DNA via groove mode and complex 2 binds more strongly to CT DNA than complex 1. Moreover, these Co(III) complexes have been found to promote the photocleavage of plasmid DNA pBR322 under irradiation at 365 nm, cytotoxicity results of complexes are also showing anticancer activity.Penumaka Nagababu, D. Aravind Kumar, Kotha Laxma Reddy, K. Ashwini Kumar, Md. B. Mustafa, Mynam Shilpa, and S. Satyanarayana© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2007/67376Three novel stable Pt(III) complexes with distorted octahedral structure and (dz2)1 ground state have been obtained in the course of Pt(II)-hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp) interaction in alkaline aqueous medium and aerobic conditions. A redox interaction also takes place together with the complexation process leading to the formation of Pt(III) species and organic radicals. The processes in the reaction system and the structure of the complexes formed cis-[Pt(III)(NH3)2(Hp−3H)(H2O)2]⋅H2O1, [Pt(III)(Hp−3H)(H2O)2]⋅H2O2, and [Pt((O,O)Hp−2H)Cl(H2O)3] 3, were studied by UV-Vis, IR, EPR and XPS spectra, thermal (TGS, DSC), potentiometric and magnetic methods. The newly synthesized complexes show promising cytotoxic activity comparable with that of cis-platin in in vitro tests against a panel of human leukemia cell lines. The observed cytotoxicity of the complex 2 against SKW-3 cells (KE-37 derivative) is due to induction of cell death through apoptosis.G. Gencheva, D. Tsekova, G. Gochev, G. Momekov, G. Tyuliev, V. Skumryev, M. Karaivanova, and P. R. Bontchev© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/2007/15925New complexes of samarium(III), gadolinium(III), and dysprosium(III) with coumarin-3-carboxylic acid (HCCA) were prepared by the reaction of the ligand with respective metal nitrates in ethanol. The structures of the final complexes were determined by means of physicochemical data, elemental analysis, IR and Raman spectra. The metal-ligand binding mode in the new Ln(III) complexes of coumarin-3-carboxylic acid was elucidated. The vibrational study gave evidence for bidentate coordination of CCA− to Ln(III) ions through the carbonylic oxygen and the carboxylic oxygen atoms. The complexes were tested for antiproliferative activitiy on the chronic myeloid leukemia-derived K-562, overexpressing the BCR-ABL fusion protein. Cytotoxicity towards tumor cells was determined for a broad concentration range. The samarium salt exerted a very weak antiproliferative effect on these cells. This is in contrast to the lanthanide complexes, especially samarium complex, which exhibited potent antiproliferative activity. The present study confirms our previous observations that the lanthanide complexes of coumarins exhibit antiproliferative activity towards K-562 cell line.Irena Kostova, Georgi Momekov, and Peya Stancheva© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/MBD.1994.1Features of pesticide synergism and acetylcholinesterase (AChE) inhibition (in vitro) were studied using a selected range of organotin compounds against the early 4th instar larvae of a highly resistant strain of the diamondback moth (DBM), Plutella xylostella, a major universal pest of cruciferous vegetables.Nazni W. Ahmad, Tay Siew Huang, S. Balabaskaran, K. M. Lo, and V. G. Kumar Das© 2008, Hindawi Publishing Corporation. All rights reserved.http://www.hindawi.com/GetArticle.aspx?doi=10.1155/MBD.1994.19A standard acute toxicity study was undertaken to assess 2′-deoxyribonucleoside cyanoboranes for therapeutic safety. 2′-Deoxyribonucleoside cyanoboranes and related derivatives were nontoxic at doses required for anti-neoplastic and hypolipidemic activities. At higher doses (50 and 100 mg/kg/day IP for 7 days), all treated animals survived with slight reductions in total body weight and small decrements in daily food consumption. No clinical chemistry value was elevated to a magnitude suggesting onset of organ specific toxicity. However, agents appeared to modulate subpopulations of white blood cells, i.e.¯, more lymphocytes than PMNs were present in blood from treated animals as determined by differential cell counts. This modulation is correlated with increases in granulomatous foci in the spleen and mesentery of treated animals after 7 days. The kidney was damaged only by Compound 5¯ at 50 and 100 mg/kg/day; Compound 5¯ had the most potent anti-neoplastic activity. The compounds demonstrated no in vitro¯ toxicity against human HCT-8 ileum cells. LD50 values were greater than 1000 mg/kg, IP, for all compounds.Iris H. Hall, Bruce S. Burnham, K. G. Rajendran, J.-J. Chang, Anup Sood, and Bernard Spielvogel© 2008, Hindawi Publishing Corporation. All rights reserved.