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Relevance. Clinical and radiological assessment mainly forms the diagnosis of periodontal diseases. The diagnosis now requires speed, sensitivity and specificity since determining the patient's disease stage is fundamental to effective treatment. Crevicular fluid biomarkers can help monitor the current state of the disease, the effectiveness of treatment, and possibly predict the pathological process progression. The combination of various biomarkers will allow maximum objectivity in periodontal tissue condition assessment.Materials and methods. The study examined 72 patients with inflammatory periodontal diseases and 25 periodontally healthy subjects. We performed a conventional clinical-instrumental examination and studied pro- and anti-inflammatory interleukins (IL-1β, IL-6, IL-17, TNF-α, VEGF, IL-8, MCP-1, IL-1RA) in the crevicular fluid. The obtained materials were processed using ROC analysis.Results. Inflammatory periodontal diseases demonstrate an increase in pro-inflammatory cytokines / chemokines (IL-1β, TNF-α, IL-6, IL-17, IL-8, MCP-1) and vascular endothelial growth factor (VEGF) in the crevicular fluid, a decrease in the anti-inflammatory cytokine, IL-1RA. The levels of pro- and anti-inflammatory cytokines, cytokines/ chemokines, VEGF are associated with the periodontal destruction severity caused by inflammation. The accumulation of VEGF, IL-6, and IL-1β in the crevicular fluid predicts the clinical course of gingivitis, VEGF, TNF-α, IL-6, IL-1β – mild and moderate periodontitis.Conclusion. The present study allows us to confirm the diagnostic value of methods for obtaining and quantifying a group of immunoregulatory cytokines in the crevicular fluid as predictors and parameters of the disease progression and the development of osteodestructive changes in the periodontium.

Relevance. The processes of osseointegration in the area of dental implant placement are accompanied by the development of reactions associ-ated with inflammation and activation of local immune processes in peri-implant tissues. Vitamin D preparations can have a significant local effect on the cells of the innate immune defense of the periodontal tissues.The aim of this work is to study the effectiveness of local application of vitamin D on the immune status of the peri-implant sulcus in rehabilitation of patients with partial secondary edentulous and chronic periodontitis by the method of dental implantation.Materials and methods.Determination of the content of biomarkers (IL-1RA, MCP-1, VEGF, TGF-β1, sTNFR) in the crevicular fluid before the installation of implants and the peri-implantation furrow fluid was carried out by the method of enzyme-linked immunosorbent assay using commercial kits «Vector Best» reagents after 3 and 6 months after surgery. The assessment of the state of the bone tissue was carried out using the Orthopantomograph tm OP300 apparatus (KAVO Dental, Germany). Vitamin D has been used topically at a therapeutic dosage.Results.Vitamin D, by reducing Th-1 and Th-17 cell proliferation and differentiation, blocks the activity of the immune-inflammatory process that occurs during implant placement.Conclusion. Application of colecalciferol in patients with moderate periodontitis leads to the activation of the production of immunoregulatory cyto-kines by the cellular structures of the peri-implantation furrow and can be used in combination with the traditional protocol in this category of patients.

The role of nitric oxide as one of the universal regulators of metabolic processes in living organisms is considered. The results of experimental studies of NO association with cancer are reviewed. Antitumor and cytotoxic effects of various nitrogen oxide donors are described and the mechanisms of their action are discussed.

A child, 5 years and 3 months old with autism spectrum disorder (ASD) and severe problem behavior was taught to stop playing and move to the learning activities. The study demonstrates the result of 2 phases of skill-based treatment (SBT) developed by Dr. Gregory Hanley: a) relinquish reinforcement phase (CAB 1) and b) transition phase (CAB 2). This is an individual case analysis, the study was conducted in a multiple baseline design across behaviors, lasted 8 weeks, and included the measurements of problem behaviors and learned skills during each training trial. As a result of 15-hour training, the child was taught the skill of stopping the play and transition to the learning area. Learners’ responses as willingness to listen to a teacher and ready to learn have emerged. At the same time, dangerous problem behavior was reduced to zero during the transition from a preferred activity to a learning area while being instructed. Transition responses were spontaneously generalized with people who were not present in the classroom (parents, tutors) and transferred to the new conditions (home and pre-school).

The cytotoxic effect of the potential antitumor drug aurumacryl (gold polyacrylate) on human skin fibroblast cell line hFB-hTERT6 has been studied in vitro. It has been found that aurumacryl exhibits substantial cytotoxicity to human skin fibroblasts. The maximum cytotoxic effect (75% cell death) is observed at an aurumacryl concentration of 0.125 mg/mL. The inhibitory concentration of aurumacryl that causes 50% human skin fibroblast death (IC50) is 0.09 mg/mL.

Relevance. The global trend associated with increasing life expectancy leads to an augmentation of the frequency of diseases and conditions associated with the cessation of estrogen production. Hormonal changes in the female body, which lead to changes in the mineral density of bone tissue, microcirculation, and immune status, create prerequisites for the destruction of target organs, including periodontal tissues. The highest prevalence of periodontal pathology is observed against the background of estrogen deficiency, especially during menopause. The multifactorial nature of the Association of pathologies that develop against the background of estrogen deficiency requires further study. Purpose. Assessment of the contribution of various pathogenetic factors to the progression of oral pathology in women in the period of reproductive aging. Materials and methods . The paper uses the results obtained during the examination of 73 patients with chronic generalized periodontitis at various stages of menopause with an assessment of the level of reproductive hormones, endothelial dysfunction, major periodontogens, and local immunity. Results. An increase in the duration of menopause leads to the formation of endothelial dysfunction, increased destruction of periodontal bone tissue, and local immunosuppression. Conclusion. The progression of periodontal diseases in menopause depends on many factors, including estrogen deficiency, violations of local and general blood supply, immunity disorders and microbial flora.

The influence of the nature of the ligands of nitric oxide-generating compounds, such as binuclear dinitrosyl iron complexes containing glutathione or mercaptosuccinate, on their tumor growth-inhibiting and cytotoxic effects has been studied in vivo and in vitro. The antitumor effect of the complex with glutathione exceeds that exerted by the complex with mercaptosuccinate. These complexes inhibit tumor growth (Lewis lung carcinoma) by 90 and 65%, respectively, compared to the control. These complexes are weakly cytotoxic against the MCF-7 human cancer cell line. The half-maximum inhibitory concentration of the complex with mercaptosuccinate at which the survival of cells is reduced by 50% (IC50) is 0.8 μmol/mL (640 μg/mL), whereas in the case of the complex with glutathione it is 2 μmol/mL (1600 μg/mL). It is assumed that the antitumor activity of iron complexes is determined by their ability to enter immunocompetent cells, which provide a direct route to tumor tissues.

Relevance. Tooth splints used to immobilize lower jaw fragments lead to the progression of periodontitis.Purpose. To study changes in periodontal tissues in patients with fractures of the lower jaw during immobilization with dentitional double jaw splints.Materials and methods. Patients with periodontitis during the treatment of fractures of the lower jaw were examined.Results. In patients with periodontitis who have a fracture of the lower jaw, inflammatory and destructive processes in periodontal tissues progress during the immobilization of fragments by the orthopedic method (tooth splints).Conclusion. Comprehensive treatment of periodontitis in fractures of the lower jaw, including dynamic magnetotherapy (DMT) and the treatment of periodontal pockets with liniment of cycloferon, reduces the severity of inflammatory and destructive processes in periodontal tissues.

—We have compared the antitumor activity of aurumacryl, a new cancer drug, and several well-known cytostatics with different mechanisms of action, that is, cisplatin, cyclophosphan, 5-fluorouracil, and doxorubicin, on experimental murine solid tumor models: Lewis lung carcinoma and Acatol adenocarcinoma. Aurumacryl is more active than the listed cytostatics except for cyclophosphan. Aurumacryl inhibits the growth of Lewis lung carcinoma and Acatol adenocarcinoma by 70 and 74%, respectively, compared to the control.

—The antitumor activity of S-nitrosoglutathione, bi- and mononuclear dinitrosyl iron complexes with different thiol-containing ligands such as glutathione, mercaptosuccinate, and thiosulfate was studied in models of transplantable murine solid tumors (Lewis lung carcinoma, Acatol adenocarcinoma, and Ca-755 adenocarcinoma). The highest antitumor activity, that is, 90% inhibition of tumor cell growth, was shown by the preparations of dinitrosyl iron complexes with glutathione via intravenous injection (Lewis lung carcinoma) and S-nitrosoglutathione via intraperitoneal injection (Ca-755 adenocarcinoma) to animals. Considering these results together with previous data on the antitumor activity of this type of compound, as well as the results of other researchers in this field, we hypothesized that the antitumor effect is mainly caused by the ability of these compounds to act as donors of nitrosonium ions. Nitrosonium ion-induced S-nitrosation of thiol-containing proteins on the surface of tumor cells leads to an increase in the intracellular oxidative capacity, thus promoting apoptosis and death of tumor cells.

The antitumor activity of the binuclear form of dinitrosyl iron complexes with mercaptosuccinate administered intravenously was studied in murine models of solid tumors: Lewis lung carcinoma and Acatol adenocarcinoma. The maximum effect, suppression of tumor growth by 65% in comparison to the control for Lewis carcinoma, was observed for a course of six intravenous injections in a daily dose of 2.5 μM/kg administered every 2 or 3 days over the period of days 1–17 after tumor transplantation.

The results of preclinical study of the original antitumor drug aurumacryl (gold polyacrylate), which belongs to polyacrylates of metals (PAMs), a new class of compounds for use in oncology, are presented. PAMs have been studied as cytostatics for the first time in the N.M. Emanuel Institute of Biochemical Physics at the Russian Academy of Sciences. The strong antitumor and cytotoxic activity of aurumacryl has been revealed. Aurumacryl induced in vivo the inhibition of growth of the murine solid tumors, as well as the death of the human tumor cells in vitro. The proliferation kinetics of the surviving fraction of tumor cells also changed after drug treatment. These alterations were expressed as the accumulation of the main part of cells in the phase of the proliferative rest and in the strong decrease of the number of proliferative cells. These data may be evaluated as the evidence of the loss of the reproductive activity by the tumor cells after aurumacryl treatment. The distribution of the aurumacryl between the tumor and some organs (blood, kidneys, liver, lungs, spleen and brain) of mice with the solid tumor has been also studied. The results of our own investigations of aurumacryl are discussed in the context of the contemporary concepts about the gold complexes antitumor effect and mechanism of action of these compounds.

The cytotoxic effect of the antitumor drug aurumacryl (gold polyacrylate) against human tumor cells of various origins has been studied. It has been shown that aurumacryl exhibits significant cytotoxic activity against cells of lung carcinoma А549 (IC50 = 60 μg/mL), melanoma Mel-mо (IC50 = 80 μg/mL), and breast carcinoma MCF-7 (IC50 = 90 μg/mL), while being substantially less efficient against colon carcinoma НСТ116 cells (IC50 = 180 μg/mL).

—Tumor cells have a higher basal ROS level than normal cells. This phenomenon may provide grounds for the development of novel antitumor drugs that are capable of selectively inducing oxidative stress in tumor cells. This approach can involve agents that induce ROS production and/or inhibit cellular enzymatic antioxidant systems. Thioredoxin reductase is a key enzyme in such systems. Overexpression of thioredoxin reductase has been shown in several types of tumors of hematopoietic, lymphoid, and other tissues. The results of studies of the antitumor activities of various synthetic and natural substances that are able to inhibit thioredoxin reductase are summarized. It is shown that thioredoxin reductase inhibition results in an increase in ROS level in tumor cells and oxidative damage of cells followed by apoptosis mainly via the mitochondrial pathway.

Aurumacryl is an incomplete metal salt of poly(acrylic acid) that exhibits hemostatic activity and inhibits the growth of transplantable carcinomas in vivo. The samples of aurumacryl synthesized following the original technique are insufficiently soluble, which complicates the study of the mechanisms involved in their synthesis and underlying their cytotoxic effect. The aim of this work was to study the impact of the following factors on aurumacryl properties: the molecular weight of the polyacrylate polymer in a range between 2 and 1,000 kDa, the presence of a counterion H+ or Na+, the molar ratio of AuCl– to the polyacrylate polymer (1 : 5 and 1 : 10), the total concentration of the polyacrylate polymer during synthesis (0.1 and 3%), and the type of drying (lyophilization). By comparing the cytotoxicity of aurumacryl samples with significantly different molar ratio of gold ions to the polyacrylate polymer against human breast carcinoma cells (MCF-7), we established that the proportion of the polymer and its molecular weight in the sample do not affect the biological properties of the synthesized substance. Using UV spectroscopy, we revealed that the concentration of Au (III) ions in aurumacryl determines its cytotoxicity.

Summary Alterations in superoxide dismutase (SOD) activity were studied on chlorotic grapevines (Vitis vinifera L.) grown under natural conditions on soil containing 30–35% CaCO3, and in lupins (Lupinus luteus L.) grown in a greenhouse with addition of 20% CaCO3 to the soil. In both series of experiments SOD activity in leaves of chlorotic plants was from 20 to 30%, higher. The efficiency and absolute rate of superoxide anion radical formation were found to rise as a result of iron deficiency in the lupin leaves. Increased SOD activity and greater amounts of enzyme isoforms were observed in the leaves of grapevine cultivars resistant to lime-induced chlorosis as compared to less resistant cultivars. The present investigation suggests that initiation of lime-induced chlorosis is determined not only by reduced chlorophyll biosynthesis but also by other consequencies of iron deficiency in tissues, particularly by the high rate of formation of superoxide and other activated oxygen species, causing destructive changes in the photosynthetic apparatus. The increased SOD activity may be regarded as a protective mechanism against the formation of superoxide.

The distribution of the antitumor drug aurumacryl (intraperitoneally injected at a dose of 100 mg/kg) in the bodies of animals with Lewis lung carcinoma was studied. The determination of aurumacryl in the tumors and organs (blood, liver, kidneys, lungs, spleen, and brain) of mice was carried out for 48 h by measuring the gold content in the test tissues using inductively coupled plasma mass spectrometry. We found the preferential accumulation of the drug in the kidneys with an extremely low gold content in the brain and a relatively uniform distribution of aurumacryl between the tumor, liver, lung, and spleen tissues.

Gold polyacrylate (aurumacryl) belonging to a new class of compounds for oncology — metal polyacrylates — was shown to exhibit strong antitumor activity. Aurumacryl causes 80—90% growth inhibition in vivo of murine solid tumors (Lewis lung carcinoma, Ca-755 adenocarcinoma, and Acatol adenocarcinoma) compared to the control and induces cell death in vitro in 60% of MCF-7 human breast carcinoma cells. Substantial changes in proliferation kinetics of the surviving fraction of tumor cells following treatment with aurumacryl were observed, which are related to the predominant accumulation (93%) of cells in the proliferative resting phase G0 and a substantial decrease in the percentage of proliferating cells (7%). These data provide evidence that the cells that survive lose reproductive ability under treatment with aurumacryl.

The interaction of the functional groups in the polyurethane foam adsorbent Penopurm® with the cations of some 3d-metals upon their extraction from aqueous solutions has been studied by atomic emission spectroscopy, UV/Vis and vibrational IR spectroscopy, and quantum chemical simulation using density functional theory. Penopurm® absorbs 3d-metal cations from aqueous solutions in the pH range 5–7. Some spectral criteria have been found indicating a predominant interaction of Ni2+ ions with various fragments of the polyurethane foam structure.

A significant antitumor activity of aqueous solutions of binuclear dinitrosyl iron complexes with glutathione was found when they were injected intravenously in a model of a solid malignant tumor, that is, Lewis carcinoma, in mice. Dinitrosyl iron complexes completely inhibited the tumor growth (by 100%) at doses of 20, 10, and 2 μmol/kg in the first 11 days after the beginning of experiment followed by tumor proliferation at a rate that was lowest for the lowest of the used doses. At day 16, the inhibition of tumor growth was 90% when a solution of dinitrosyl iron complexes was injected at a dose of 2 μmol/kg five times with an interval of 2 to 3 days between injections; whereas the inhibition of tumor growth did not exceed 70 and 30% at doses of 10 and 20 μmol/kg, respectively. Acceleration, rather than inhibition of carcinoma growth was observed at a dose of 100 μmol/kg. The tumor weight increased 1.5–2.0 times compared to the control values, depending on the time.

The cellular effects of aurumacryl (a drug based on gold polyacrylate, which previously showed significant antitumor activity in vivo against solid tumors in mice) were studied in the model of the MCF7 stable cell line of human breast carcinoma. It was found that aurumacryl possesses cytotoxic and cytostatic effects on tumor cells. The dose-dependent cytotoxic effect of aurumacryl is expressed as the death of 60% of tumor cells after incubation with aurumacryl at a dose of 1 mg/mL for 24 h. The proliferation kinetics of the surviving fraction of tumor cells also undergoes significant changes, which is expressed in the predominant accumulation of the cells (93%) in the G0 phase of proliferative rest and in a significant decrease in the number of proliferating cells to 7%. These data could be interpreted as evidence of the loss of the reproductive ability of the surviving cells after treatment with aurumacryl.

The hemostatic activity of polymeric gold and silver nanocomposites depends on their kinetic stability caused by the interaction of the ligand with nanoparticles. The properties of the nanoparticles are determined by the metal nature.

The antitumor activity of the binuclear form of dinitrosyl iron complexes with glutathione against Lewis lung carcinoma was found earlier with intraperitoneal administration of the complexes. This activity was also observed when this preparation was injected subcutaneously. The complex inhibited the tumor growth by 43% upon subcutaneous injection at a daily dose of 100 µM/kg (as calculated per one iron atom in the binuclear dinitrosyl iron complex) for 10 or 15 days. The effect was observed during the first 2 weeks after tumor transplantation. After this, the tumors began to grow at a rate that was equal to or even higher than that for the control animals. The mean survival time for the treated mice exceeded the control values by 30%. Binuclear dinitrosyl iron complexes were also effective against Ca-755 adenocarcinoma with intraperitoneal administration. In this case, however, the mean survival time for the treated animals only increased by 7%. It was also shown that S-nitrosoglutathione inhibited the growth of Lewis lung carcinoma and Ca-755 adenocarcinoma by 70 and 90%, respectively. However, in contrast to binuclear dinitrosyl iron complexes, the antitumor effect of S-nitrosoglutathione decreased with an increase in the daily dose of the compound from 200 to 400 µM/kg. The initial antitumor effect of binuclear dinitrosyl iron complexes and S-nitrosoglutathione is suggested to be due to NO that is released from both compounds. The subsequent suppression of the effect is caused by the activation of antinitrosative and antioxidant defense systems in tumors.

Physicomechanical and electrophysical characteristics of a polyurethane composite doped with carbon-containing materials have been investigated. It has been found that the roughness of the sample’s surface and also the porosity increase with the concentration of the dopant. Volt-ampere characteristics of composite materials point to the activated type of conductivity in these materials; however, at a temperature of nearly 340 K, the type of conductivity is changed. Also, the frequency dependence of the conductivity has been established.

The antitumor effect of a polymer of aspartic acid, polysuccinimide, against murine solid-tumor models, such as Lewis lung carcinoma, AKATOL adenocarcinoma, and Ca-755 adenocarcinoma was found. The tumor growth inhibition was 60–80% compared to the control. The antimetastatic activity of polysuccinimide was found; in the Lewis lung carcinoma model it manifests itself in inhibition of lung metastases by 60% compared to the control. It was shown that polysuccinimide does not shift the pH values of tumors (P-388 lympholytic leukemia, AKATOL adenocarcinoma) into the region of acidic values. The experimental study indicates the advisability of further profound preclinical trials of the antitumor properties and mechanism of action of polysuccinimide.

Inhibition of growth of a transplanted solid tumor in BDF1 mice bearing Lewis lung carcinoma cells on days 1–5 and 7–11 after tumor transplantation was observed at daily intraperitoneal administration of an aqueous solution of binuclear form of dinitrosyl iron complexes with glutathione at a dose of 200 μmol/kg (relative to one Fe(NO)2 group in the complexes). Inhibition of tumor growth during the administration of complexes (for 11 days) was 70 and 85% when an iron complex: free glutathione ratio in solution was equal to 1: 1 and 1: 10, respectively. Accelerated tumor growth that was faster than in the control began after cessation of dinitrosyl iron complex administration. The selective accumulation of dinitrosyl iron complexes in the tumor, as well as the accumulation of nitrosyl complexes of heme proteins was detected by the EPR method. The latter were observed in the tumor and control animals. It is hypothesized that delayed tumor development during administration of the binuclear form of dinitrosyl iron complexes to mice is caused by inactivation of heme-containing proteins under the action of NO released from these complexes, which provides antinitrosative defenses produced in malignant tumors.

We analyzed the research data on antitumor effects of a wide range of ferrocene compounds and discussed possible mechanisms of their bioactivities. Current trends in the study of anticancer effects of ferrocene derivatives were considered. Promising ways in the design of low-toxicity anticancer ferrocene-based drugs of new generation were outlined.

Compounds belonging to three novel groups of oncological drugs (metal polyacrylates, ferrocene derivatives, and polysuccinimide) showed antitumor activity. The most efficient compounds, viz., gold polyacrylate (auracryl), 2-[(1-ferrocenylethyl)sulfanyl]pyrimidine (LS-17), and polysuccinimide, inhibit the growth of murine solid tumors by 70–95% and are recommended for further thorough preclinical studies of their antitumor properties and mechanisms of action.

The antitumor dose-dependent effect of binuclear dinitrosyl iron complexes with glutathione as NO donors on a solid tumor in the mouse, Lewis lung carcinoma, was detected. The complexes being injected at doses of 21, 42, 105 mg/kg daily for 10 days blocked completely the development of the tumor for the first week after tumor cell implantation into animals. After that, the part of tumor cells which remained in intact alive state began to grow at a rate equal to that for control animals. The effect was proposed to be caused via formation of an antinitrosative defense system in the cells as a response to NO attack on cells. It was also hypothesized that this system can be inactivated by higher doses of dinitrosyl iron complexes. Data were obtained which were in line with the hypothesis.

The peculiarities of wettability of diamond that was obtained in a nanostructured form as ultrananocrystalline diamond (UNCD) films by deposition from a gas phase are considered. Surface hydrogenation leads to hydrophobicity: advancing contact angle θ for UNCD films reaches 106 ± 1° (for diamond single crystals θ = 93°). Even higher values of θ equal to 124 ± 3° were detected for nanoporous samples of UNCD, in which a graphite-like component was removed by etching. High hydrophobicity is achieved owing to the specific surface morphology of the nanostructured diamond (anisotropic, with high content of nanopores) and chemical modification, which on the whole provides for very low values of free surface energy of the films. It was shown that laser-drilled microholes in polycrystalline diamond also can enhance the hydrophobicity. The wetting behavior of the nanostructured surfaces agrees well with the Cassie-Baxter equation for heterophase porous surfaces. The oxidation and hydrogenation of UNCD films allows controlling of θ in considerably wider ranges compared to single crystal diamond.

The anti-tumor activity of the binuclear form of dinitrosyl iron complexes with glutathione against Lewis lung carcinoma, found earlier upon intraperitoneal administration of the complexes, was also observed when this preparation was injected subcutaneously. A 100 μM/kg subcutaneous dose of the complex being used daily (as calculated per one iron atom in binuclear dinitrosyl iron complexes) for 10 or 15 days, inhibited the tumor growth by 43%. The effect was observed during the first two weeks after tumor transplantation. After that, the tumors began to grow at the rate equal to or even higher than that one for control animals. The mean survival time for treated mice exceeded the control values by 30%. Binuclear dinitrosyl iron complexes administered intraperitoneally was also effective against Ca-755 adenocarcinoma. However, in this case the mean survival time for treated animals increased only by 7%. The anti-tumor activity of S-nitrosoglutathione against Lewis lung carcinoma growth inhibition by 70% and Ca-755 adenocarcinoma growth inhibition by 90% was also shown. However, unlike binuclear dinitrosyl iron complexes the anti-tumor effect of S-nitrosoglutathione decreased when a daily dose of the compound increased (from 200 to 400 μM/kg) The initial anti-tumor effect of binuclear dinitrosyl iron complexes and S-nitrosoglutathione is suggested to be due to NO released from both compounds. A subsequent suppression of the effect is determined by the development of anti-nitrosative and anti-oxidant defense systems in tumors.

The case of clinical supervision of the patient having polimorbid pathology is presented. One of extraesophageal manifestations of a gastroesophageal reflux disease is the glossalgia. Glossalgia is the polyetiological disease. Treatment needs to be carried out taking into account the factors causing emergence of a glossalgia. In this regard normalization of functions of organs and systems of an organism is provided.

Ferrocenylalkyl thiopyrimidines (6a–d to 9a–d) were prepared via the reaction of the α-(hydroxy)alkyl ferrocenes, FcCHR(OH) (1a–d; Fc = ferrocenyl; R = H, Me, Et, Ph), with 2-thiopyrimidines (2–5) in acetone at room temperature in the presence of TFA, yielding 50–95%. The resulting enantiomers were resolved using HPLC on modified cellulose as chiral selector. The antitumor activities of S-ferrocenylethyl 2-thiopyrimidine (6b) against two murine solid tumor models, carcinoma 755 (Ca755) and Lewis lung carcinoma (LLC) were evaluated in vivo. The strong antitumor effect of compound 6b on Ca755 and LLC was demonstrated. The index of tumor growth inhibition on Ca755 equaled 95% in comparison with control. Copyright © 2010 John Wiley & Sons, Ltd.

Data on the antitumor activities of ferrocene compounds and the results concerning the mechanisms of their action published between 1995 and 2010 are discussed. The biomedical aspects of the study of ferrocene derivatives are briefly analyzed.

Ferrocenylalkyl nucleobases (1–14) were prepared via the reaction of the α-(hydroxy)alkyl ferrocenes FcCHR(OH) (Fc = ferrocenyl; R = H, Me, Et, Ph) with thymine, cytosine, iodo-cytosine and adenine in DMSO at 100 °C, yields being 50–80%. The antitumor activities of ferrocenylmethyl thymine (1) against solid tumor models, carcinoma 755 (Ca755) and Lewis lung carcinoma (LLC) were studied in vivo. Therapeutic synergism of antitumor activity against LLC was demonstrated in the case of combined application of compound 1 with anticancer drug cyclophosphamide. Copyright © 2009 John Wiley & Sons, Ltd.

The antitumor activity of o-carboxybenzoylferrocene sodium salt (1) was studied in vivo. Interaction between o-carboxybenzoylferrocene (2) and N,N′-carbonyldiimidazole in boiling methylene dichloride leads to 3-(N-imidazolyl)-3-ferrocenylisobenzofuran-1(3H)-one (5). The structure of compound 5 was established by X-ray analysis. Aminolysis of compound 5 in toluene gave rise to ferrocenoylbenzamides (6a–d)–derivatives of dimethylamine, piperidine, pyrrolidine and morpholine. Copyright © 2008 John Wiley & Sons, Ltd.