Synthesis of Prostate-Specific Membrane Antigen-Targeted Bimodal Conjugates of Cytotoxic Agents and Antiandrogens and Their Comparative Assessment with Monoconjugates.

Prostate cancer is the second most common cancer among men. We designed and synthesized new ligands targeting prostate-specific membrane antigen and suitable for bimodal conjugates with diagnostic and therapeutic agents. studies of the affinity of the synthesized compounds to the protein target have been carried out.

Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.

We report an improved series of ligands targeting prostate specific membrane antigen (PSMA). The new compounds were designed by the introduction of changes in the structure of the aromatic fragment at ε-nitrogen atom of lysine that resulted in improved biological parameters. Some of them demonstrated high selectivity and nanomolar IC values.

Thiourea Modified Doxorubicin: A Perspective pH-Sensitive Prodrug.

A novel approach to the synthesis of pH-sensitive prodrugs has been proposed: thiourea drug modification. Resulting prodrugs can release the cytotoxic agent and the biologically active 2-thiohydantoin in the acidic environment of tumor cells. The concept of acid-catalyzed cyclization of thioureas to 2-thiohydantoins has been proven using a FRET model.

Correction: New ferrocene-based 2-thio-imidazol-4-ones and their copper complexes. Synthesis and cytotoxicity.

Correction for 'New ferrocene-based 2-thio-imidazol-4-ones and their copper complexes. Synthesis and cytotoxicity' by D. A.

New ferrocene-based 2-thio-imidazol-4-ones and their copper complexes. Synthesis and cytotoxicity.

Synthesis, characterization (HRMS, NMR, EPR, XANES, UV-Vis spectroscopy, and electrochemistry), DNA and BSA binding and in vitro biological screening of two new ferrocene-incorporated thiohydantoin derivatives (5 and 6) and their copper coordination compounds are reported. The ferrocene-based thiohydantoin derivatives were prepared by copper-catalyzed azide alkyne cycloaddition reactions between alkynyl ferrocenes and 5-(Z)-3-(2-azidoethyl)-2-(methylthio)-5-(pyridin-2-ylmethylene)-1H-imidazol-4H-one. Alkynyl ferrocenes necessary for these syntheses were prepared by new procedures.

[The association between the 5-HTTLPR polymorphism of the serotonin transporter gene and the efficacy and tolerability of selective serotonin reuptake inhibitors].

Objective: To search for the association between the 5-HTTLPR polymorphism of the serotonin transporter gene and the efficacy and tolerability of selective serotonin reuptake inhibitors (SSRIs).

Material And Methods: The complex clinical/psychopathological and genetic study of 38 patients with depression treated with SSRIs was carried out.

Results And Conclusion: The 5-HTTLPR polymorphism was associated with the rate of achievement of remission and tolerability of treatment: carriers of the SS genotype achieved remission less frequently and more frequently experienced side-effects.

[The kidney transplantation from the ABO-incompatible donors].

The experience of 28 allotransplantations of ABO-incompatible kidneys was compared with the treatment results of 38 ABO-compatible renal transplantations. The transplanted kidney function, morphological changes of the transplanted kidney and the comparative analysis of actuary survival in both groups showed no significant difference. The results of the study prove the validity of the kidney transplantation from the ABO-incompatible donors.

[Significance of the isoantigen A2 and immune anti-A1 antibodies in transfusiology].

The paper gives data on the frequency of A2 and A2B blood groups in the blood samples of 3590 donors and patients and on the carriage of irregular anti-A1 antibodies. To define the belonging of anti-A1 antibodies to various classes of immunoglobulins, their resistance and temperature optimum, at which the antibodies showed the highest activity, the authors examined the irregular anti-A1 antibodies-containing sera from 43 subjects with A2 and A2B blood groups. The necessity of identifying the carriage of irregular anti-A1 antibodies is determined by the fact that there may be posttransfusion reactions or complications in recipients, the carriers of such antibodies, who are transfused donor red blood cells containing the antigen A1.

[Diagnostic value of the radioimmunoassay and immunoenzyme assay in analysis of HBsAg in children with viral hepatitis].

The purpose of the case study was to evaluate the diagnostic efficiency of radioimmunoassay (RIA) and of immune-enzyme assay (IEA) in indicating the HBsAg in the blood of children with viral hepatitis. The study was based on a simultaneous indication of HBsAg by RIA and IEA in 98 samples of blood serum (plasma). It was shown that both assays are practically univocal in as far as the HBsAg indication within the mentioned circumstances is concerned.

[A method of immunoenzyme analysis for determining human histocompatibility antigens].

Enzyme immunoassay (EIA) has been applied to measurements of human histocompatibility (HLA) antigens (antibodies). The optimal concentration of the antigen immobilized on solid phase and the optimal dilutions of HLA sera have been found. The assays have been performed with the peripheral blood lymphocytes and platelets from donors with a known HLA phenotype.

[Fecundity of Aedes aegypti mosquitoes in relation to their infection with the malaria agent Plasmodium gallinaceum].

Studies of the effect of P. gallinaceum on Ae. aegypti in different periods of the agent's sporogony and during different gonotrophic cycles of the vector have shown the absence of strong inhibition of mosquitoes' fecundity.