ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDiastereomers of Nucleoside 3'-O-(2-Thio-1,3,2-oxathia(selena)phospholanes): Building Blocks for Stereocontrolled Synthesis Oligo(nucleoside phosphorothioate)sWojciech J. Stec, Andrzej Grajkowski, Anna Kobylanska, Boleslaw Karwowski, Maria Koziolkiewicz, Konrad Misiura, Okruszek, Wilk, Piotr Guga, and Malgorzata BoczkowskaCite this: Am. Chem. Soc. 1995, 117, 49, 12019–12029Publication Date (Print):December 1, 1995Publication History Published...

We have designed novel tropinone-thiazole derivatives that showed high antiproliferative activity against a variety of cancer cell lines via caspase 3/7 activation mechanism. Among the derivatives, compounds 3b-3h were found to exhibit human leukemia (MV4-11), lung carcinoma (A549), breast (MCF-7), and skin melanoma (B16-F10) lines, with IC50 values 5.43-11.06 μM. The lead compound 3g increases in A549 cells 25 times more than control, 2 reference drug camptothecin. also tyrosinase...

Non-nucleosidic phosphoramidite linker units suitable for use on commercial DNA synthesis machines have been designed the direct incorporation of biotin and a new reporter group, phosphotyrosine, at multiple sites synthetic oligonucleotides. The are based 3-carbon glyceryl backbone where group is attached to 2-O-position through 3-aminopropyl spacer. 17-mer oligonucleotides were synthesized carrying 5'-end 1, 2, 4 or 8 biotinyl phosphotyrosinyl respectively used detection nitrocellulose...

Synthesis and investigation of antimicrobial activity 22 novel thiazoles selenazoles derived from dihydro-2H-thiopyran-4(3H)-one are presented. Additionally, anticonvulsant six derivatives is examinated. Among the derivatives, compounds 4a-f, 4i, 4k, 4 l, 4n, 4o-s 4v have very strong against Candida spp. with MIC = 1.95-15.62 μg/ml. In case 4o, 4r 4s, some strains isolated clinical materials, 0.98 to 15.62 4n-v found be active Gram-positive bacteria 7.81-62.5 The results screening reveal...

Synthesis, characterization and investigation of in vivo anticonvulsant activities 13 novel cyclopentanecarbaldehyde-based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using (1)H (13)C NMR, FAB(+)-MS, HRMS elemental analyses. The results screening reveal that seven intraperitoneally administered compounds: 3a, 3b, 3d, 3e, 3f, 3k 3m containing F-, Cl-, Br-, CF3-, CH3- adamantyl substituents demonstrated significant activity the pentylenetetrazole model with...

Synthetic oligonucleotides and their chemical modifications have been shown to inhibit viral cellular gene expression by sequence-specific antisense hybridization target mRNAs. We now report that oligodeoxynucleotide phosphorothioates nuclease-resistant are effective in micromolar submicromolar concentrations against the growth of both chloroquine-resistant chloroquine-sensitive strains Plasmodium falciparum vitro. Parasitized human erythrocytes were found be accessible radioactively labeled...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStereospecific synthesis of chiral metabolites ifosfamide and their determination in the urineK. Misiura, A. Okruszek, K. Pankiewicz, W. J. Stec, Z. Czownicki, B. UtrackaCite this: Med. Chem. 1983, 26, 5, 674–679Publication Date (Print):May 1, 1983Publication History Published online1 May 2002Published inissue 1 1983https://pubs.acs.org/doi/10.1021/jm00359a010https://doi.org/10.1021/jm00359a010research-articleACS PublicationsRequest reuse...

A new series of hybrid compounds with tropinone and thiazole rings in the structure was designed synthesized as potential anticancer agents. They were tested against human multiple myeloma (RPMI 8226), lung carcinoma (A549), breast adenocarcinoma (MDA-MB-231), mouse skin melanoma (B16-F10) cell lines. Toxicity on normal fibroblasts (HSF) colon (CCD-18Co). The growth inhibition mechanism most active derivative analyzed through investigation its effect distribution cycle phases ability to...

Synthesis, characterization and investigation of antibacterial antifungal activities twelve camphor based 2,4-disubstituted 1,3-thiazoles is presented. Their structures were determined using NMR, IR, FAB MS HRMS analyses. Among the derivatives, 3i 5 found to exhibit comparable that fluconazole ciprofloxacin against yeast belonging Candida spp., MIC 0.12-0.98 μg/ml Gram-positive bacteria including both pathogenic S. aureus opportunistic epidermidis, 0.98-7.81 μg/ml, B. subtilis cereus,...

Synthesis, characterization and investigation of antiproliferative activity eight thiazole-based nitrogen mustard against human cancer cells lines (MV4-11, A549, HCT116 MCF-7) normal mouse fibroblast (BALB/3T3) are presented. Their structures were determined using NMR, FAB MS, HRMS elemental analyses. Among the derivatives, 3a, 3b, 3e 3h found to exhibit high leukemia MV4-11 with IC50 values 0.634-3.61 µg/ml. The cytotoxic compound 3a BALB/3T3 is up 40 times lower than cell lines. Our data...

Background: Synthesis, characterization and investigation of antibacterial activity ten novel Schiff base derivatives 4-formylbenzoic acid is presented. Their structures were determined using 1H 13C NMR, EI(+)-MS elemental analyses. Additionally, DFT calculations interaction energies in complexes the drugs DNA bases are carried out. Objective: Design synthesis thiazole with benzoic scaffold to obtain compounds an improved activity. Method: The examined screened vitro for broth microdilution...

Synthesis, characterization and investigation of antifungal antibacterial activities fourteen 2,4- disubstituted 1,3-selenazoles is presented. Their structures were determined using 1H 13C NMR, FAB MS HRMS analyses. Among the derivatives, compounds 5, 6, 8, 9, 12, 13 15 had very strong activity against reference strains C. albicans ATCC 10231 parapsilosis 22019 with MIC = 0.24-7.81 µg/ml. The showed also clinical isolates belonging to non-albicans Candida spp. strains, i.e. krusei,...

Nucleoside 5'-O-(α-thiotriphosphates) were obtained in reactions of the appropriate nucleoside 5'-O-(2-thio-1,3,2-oxathiaphospholanes) with pyrophosphate presence DBU. The presented method allows also for preparation α-seleno congeners and corresponding α-modified diphosphates.

The aim of this study was to evaluate the impact GSTM1, GSTT1, and GSTP1 gene polymorphism on urinary excretion unchanged ifosfamide, 2-dechloroethylifosfamide (2DCIF), 3-dechloroethylifosfamide (3DCIF) with regard incidence ifosfamide-related nephrotoxicity neurotoxicity in children. comprised 76 children (38 girls, 38 boys) ages 9.84 210 months who were being treated for various malignant diseases ifosfamide. enrolled after identification genotype coding three classes glutathione...

Synthesis, characterization and investigation of antibacterial antifungal activities thirteen novel 6- hydroxybenzofuran-3(2H)-one based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using NMR, FAB MS HRMS analyses. The results microbiological screening reveal that three derivatives containing fluorine, bromine hydrogen substituents at the phenyl ring most active antimicrobial compounds. Molecular docking studies all compounds on sites microbial enzymes...

A series of 3-(2-chloroethyl)-N-(2-X-ethyl)tetrahydro-2H-1,3,2-oxazaphosphorin -2-amine 2-oxides with various X substituents have been prepared by cyclization racemic ifosfamide or its enantiomers sodium hydride and subsequent treatment intermediary products hydrobromic acid, diethyl hydrogen phosphate, dibenzyl p-toluenesulfonic acetic acid. All these compounds were tested in vivo against L 1210 lymphoid leukemia mice. Only bromo analogue 13 effective, exceeding the activity...

It is shown that enantiomers and racemates have identical isotropic NMR chemical shift as well anisotropic chemical-shift tensor parameters can be easily distinguished by means of the ODESSA (One Dimensional Exchange Spectroscopy Sideband Alternation) technique. The method based on fact molecular symmetries packing are usually significantly different. power proposed approach demonstrated employing model compounds P-chiral oxazaphosphorine derivatives, which widely used in clinical oncology....

Abstract Synthesis, characterization and investigation of antimicrobial activities seven new 6-(1,3-thiazol-4-yl)-1,3-benzoxazol-2(3 H )-ones are presented. Their structures were determined using 1 NMR, 13 C NMR elemental analyses. The compounds possess some biological activity against Gram-positive bacteria, especially Micrococcus luteus belonging to opportunistic pathogens, with an MIC 31.25 μg/mL.

ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTThe First Stereocontrolled Solid-Phase Synthesis of Di-, Tri-, and Tetra[adenosine (2',5') phosphorothioate]sXian-Bin Yang, Agnieszka Sierzchała, Konrad Misiura, Wojciech Niewiarowski, Marek Sochacki, J. Stec, Michał W. WieczorekView Author Information Polish Academy Sciences, Centre Molecular Macromolecular Studies, Department Bioorganic Chemistry, Sienkiewicza 112, 90-363 Łódź, Poland, Institute General Food Technical University Stefanowskiego 4/10,...

The relationship between enantiomeric homogeneity of three oxazaphosphorine drugs: cyclophosphamide, ifosfamide and trofosfamide their antitumor activity was evaluated by standard screening tests against four in vivo transplantable tumor models: L 1210 P 388 lymphoid leukemias, Lewis lung carcinoma 16/C line mouse mammary adenocarcinoma. It shown that the stereodifferentiation anti-tumor effect enantiomers not outstanding although quite consistently favor levorotatory forms. only exception...