Synthesis and Inhibition Activity Study of Triazinyl-Substituted Amino(alkyl)-benzenesulfonamide Conjugates with Polar and Hydrophobic Amino Acids as Inhibitors of Human Carbonic Anhydrases I, II, IV, IX, and XII.

Primary sulfonamide derivatives with various heterocycles represent the most widespread group of potential human carbonic anhydrase (hCA) inhibitors with high affinity and selectivity towards specific isozymes from the hCA family. In this work, new 4-aminomethyl- and aminoethyl-benzenesulfonamide derivatives with 1,3,5-triazine disubstituted with a pair of identical amino acids, possessing a polar (Ser, Thr, Asn, Gln) and non-polar (Ala, Tyr, Trp) side chain, have been synthesized. The optimized synthetic, purification, and isolation procedures provided several pronounced benefits such as a short reaction time (in sodium bicarbonate aqueous medium), satisfactory yields for the majority of new products (20.

Advances in Development of Radiometal Labeled Amino Acid-Based Compounds for Cancer Imaging and Diagnostics.

Radiolabeled biomolecules targeted at tumor-specific enzymes, receptors, and transporters in cancer cells represent an intensively investigated and promising class of molecular tools for the cancer diagnosis and therapy. High specificity of such biomolecules is a prerequisite for the treatment with a lower burden to normal cells and for the effective and targeted imaging and diagnosis. Undoubtedly, early detection is a key factor in efficient dealing with many severe tumor types.

Synthetic Strategies and Computational Inhibition Activity Study for Triazinyl-Substituted Benzenesulfonamide Conjugates with Polar and Hydrophobic Amino Acids as Inhibitors of Carbonic Anhydrases.

Various sulfonamide derivatives are intensively studied as anticancer agents owing to their inhibitory activity against human tumor-associated carbonic anhydrase isoforms. In this work, different synthetic procedures for the series of 1,3,5-triazinyl-aminobenzenesulfonamide conjugates with amino acids, possessing polar uncharged, negatively charged, and hydrophobic side chain, were studied and optimized with respect to the yield/purity of the synthesis/product as well as the time of synthetic reaction. These procedures were compared to each other via characteristic HPLC-ESI-DAD/QTOF/MS analytical product profiles, and their benefits as well as limitations were discussed.

Novel sulfonamides incorporating 1,3,5-triazine and amino acid structural motifs as inhibitors of the physiological carbonic anhydrase isozymes I, II and IV and tumor-associated isozyme IX.

A new series of thirty s-triazinyl-substituted aminoalkylbenzenesulfonamides, incorporating a symmetric pair of amino acid moieties, is reported, together with inhibition studies of physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.

Prevention of irinotecan induced diarrhea by probiotics: A randomized double blind, placebo controlled pilot study.

Purpose: Diarrhea is one of the dose limiting toxicity of irinotecan. SN-38 is main irinotecan metabolite responsible for diarrhea development, which is excreted in glucuronidated form into the intestine. This study aimed to determine the effectiveness of the probiotics in the prevention of irinotecan induced diarrhea due to reduction of intestinal beta-d-glucuronidase activity.

Analysis of radiation-induced angiosarcoma of the breast.

Breast angiosarcoma may occur de novo, or as a complication of radiation therapy, or chronic lymphedema secondary to axillary lymph node dissection for mammary carcinoma. Both primary and secondary angiosarcomas may present with bruise like skin discoloration, which may delay the diagnosis. Imaging findings are nonspecific.

Bevacizumab in combination with chemotherapy in the first-line treatment of metastatic colorectal carcinoma.

Colorectal carcinoma (CRC) is a malignancy of worldwide increased incidence. The vast majority of all CRC cases occur in patients older than age 50. The initial stage at the time of diagnosis has a strong influence on the overall survival (OS).

[Verification of identification of infectious agents by culture in routine gynecologic cytological screening].

The original Bethesda classification system for reporting cervical/vaginal cytologic diagnoses has claimed besides oncologic evaluation also a statement on the presence of infectious agents. Their diagnosis should be followed by appropriate treatment. Based upon the comparison of careful bacterioscopic study in a series of 175 routine cervical smears with the results of microbiological, virological and mycological examinations the following pathogens might be-according to the authors' opinion-diagnosed as highly possible and recommended for laboratory verification: cocci, Gardnerella vaginalis, Klebsiella, Acinetobacter, Morganella Morgani, Candida, Trichomonas vaginalis, Chlamydia trachomatis and human papilloma virus.

[Urethritis of chlamydial origin].

Using the direct immunofluorescence method with a Chlamyset of Orion Co. Finland for detection of Chlamydia trachomatis, the authors examined smears from male and female patients with manifestations of non-specific urethritis and cervicitis. In women also specimens from the cervix were examined.