LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 4 of total 4

Search options

  1. Article ; Online: Experimental and Theoretical Analysis of the Thiol-Promoted Fragmentation of 2-Halo-3-tosyl-oxanorbornadienes.

    Carranza, Marina / Carmona, Ana T / Navo, Claudio D / Robina, Inmaculada / Fratta, Simone / Newburn, Carlos / Jiménez-Osés, Gonzalo / Moreno-Vargas, Antonio J

    Organic letters

    2023  Volume 25, Issue 41, Page(s) 7481–7485

    Abstract: 2-Halo-3-tosyl-oxanorbornadienes are able to accept two thiol molecules through an initial nucleophilic substitution, giving isolable oxabicyclic thiovinyl sulfones that, subsequently, can react with a second thiol molecule via thio-Michael addition. The ...

    Abstract 2-Halo-3-tosyl-oxanorbornadienes are able to accept two thiol molecules through an initial nucleophilic substitution, giving isolable oxabicyclic thiovinyl sulfones that, subsequently, can react with a second thiol molecule via thio-Michael addition. The resulting oxanorbornenic thioketals undergo retro-Diels-Alder (rDA) fragmentation to release a furan derivative and a ketene
    Language English
    Publishing date 2023-10-10
    Publishing country United States
    Document type Journal Article
    ISSN 1523-7052
    ISSN (online) 1523-7052
    DOI 10.1021/acs.orglett.3c02548
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  2. Article ; Online: Synthesis and structure-activity relationship of new nicotinamide phosphoribosyltransferase inhibitors with antitumor activity on solid and haematological cancer.

    Fratta, Simone / Biniecka, Paulina / Moreno-Vargas, Antonio J / Carmona, Ana T / Nahimana, Aimable / Duchosal, Michel A / Piacente, Francesco / Bruzzone, Santina / Caffa, Irene / Nencioni, Alessio / Robina, Inmaculada

    European journal of medicinal chemistry

    2023  Volume 250, Page(s) 115170

    Abstract: Cancer cells are highly dependent on Nicotinamide phosphoribosyltransferase (NAMPT) activity for proliferation, therefore NAMPT represents an interesting target for the development of anti-cancer drugs. Several compounds, such as FK866 and CHS828, were ... ...

    Abstract Cancer cells are highly dependent on Nicotinamide phosphoribosyltransferase (NAMPT) activity for proliferation, therefore NAMPT represents an interesting target for the development of anti-cancer drugs. Several compounds, such as FK866 and CHS828, were identified as potent NAMPT inhibitors with strong anti-cancer activity, although none of them reached the late stages of clinical trials. We present herein the preparation of three libraries of new inhibitors containing (pyridin-3-yl)triazole, (pyridin-3-yl)thiourea and (pyridin-3/4-yl)cyanoguanidine as cap/connecting unit and a furyl group at the tail position of the compound. Antiproliferative activity in vitro was evaluated on a panel of solid and haematological cancer cell lines and most of the synthesized compounds showed nanomolar or sub-nanomolar cytotoxic activity in MiaPaCa-2 (pancreatic cancer), ML2 (acute myeloid leukemia), JRKT (acute lymphobalistic leukemia), NMLW (Burkitt lymphoma), RPMI8226 (multiple myeloma) and NB4 (acute myeloid leukemia), with lower IC
    MeSH term(s) Humans ; Nicotinamide Phosphoribosyltransferase/metabolism ; NAD/metabolism ; Cell Line, Tumor ; Cytokines/metabolism ; Antineoplastic Agents/pharmacology ; Leukemia/metabolism ; Structure-Activity Relationship ; Hematologic Neoplasms/drug therapy ; Enzyme Inhibitors/pharmacology
    Chemical Substances Nicotinamide Phosphoribosyltransferase (EC 2.4.2.12) ; NAD (0U46U6E8UK) ; Cytokines ; Antineoplastic Agents ; Enzyme Inhibitors
    Language English
    Publishing date 2023-01-31
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2023.115170
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  3. Article: Structure-Based Identification and Biological Characterization of New NAPRT Inhibitors.

    Franco, Jorge / Piacente, Francesco / Walter, Melanie / Fratta, Simone / Ghanem, Moustafa / Benzi, Andrea / Caffa, Irene / Kurkin, Alexander V / Altieri, Andrea / Herr, Patrick / Martínez-Bailén, Macarena / Robina, Inmaculada / Bruzzone, Santina / Nencioni, Alessio / Del Rio, Alberto

    Pharmaceuticals (Basel, Switzerland)

    2022  Volume 15, Issue 7

    Abstract: NAPRT, the rate-limiting enzyme of the Preiss-Handler NAD biosynthetic pathway, has emerged as a key biomarker for the clinical success of NAMPT inhibitors in cancer treatment. Previous studies found that high protein levels of NAPRT conferred resistance ...

    Abstract NAPRT, the rate-limiting enzyme of the Preiss-Handler NAD biosynthetic pathway, has emerged as a key biomarker for the clinical success of NAMPT inhibitors in cancer treatment. Previous studies found that high protein levels of NAPRT conferred resistance to NAMPT inhibition in several tumor types whereas the simultaneous blockade of NAMPT and NAPRT results in marked anti-tumor effects. While research has mainly focused on NAMPT inhibitors, the few available NAPRT inhibitors (NAPRTi) have a low affinity for the enzyme and have been scarcely characterized. In this work, a collection of diverse compounds was screened in silico against the NAPRT structure, and the selected hits were tested through cell-based assays in the NAPRT-proficient OVCAR-5 ovarian cell line and on the recombinant hNAPRT. We found different chemotypes that efficiently inhibit the enzyme in the micromolar range concentration and for which direct engagement with the target was verified by differential scanning fluorimetry. Of note, the therapeutic potential of these compounds was evidenced by a synergistic interaction between the NAMPT inhibitor FK866 and the new NAPRTi in terms of decreasing OVCAR-5 intracellular NAD levels and cell viability. For example, compound IM29 can potentiate the effect of FK866 of more than two-fold in reducing intracellular NAD levels. These results pave the way for the development of a new generation of human NAPRTi with anticancer activity.
    Language English
    Publishing date 2022-07-12
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph15070855
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  4. Article ; Online: Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2.

    Højgaard Hansen, Anders / Christensen, Henriette B / Pandey, Sunil K / Sergeev, Eugenia / Valentini, Alice / Dunlop, Julia / Dedeo, Domonkos / Fratta, Simone / Hudson, Brian D / Milligan, Graeme / Ulven, Trond / Rexen Ulven, Elisabeth

    ChemMedChem

    2021  Volume 16, Issue 21, Page(s) 3326–3341

    Abstract: Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, ... ...

    Abstract Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB (1). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.
    MeSH term(s) Amides/chemical synthesis ; Amides/chemistry ; Amides/pharmacology ; Animals ; Dose-Response Relationship, Drug ; Drug Discovery ; Humans ; Mice ; Molecular Structure ; Phenylbutyrates/chemical synthesis ; Phenylbutyrates/chemistry ; Phenylbutyrates/pharmacology ; Receptors, Cell Surface/antagonists & inhibitors ; Receptors, Cell Surface/metabolism ; Structure-Activity Relationship
    Chemical Substances Amides ; FFA2R protein, human ; Phenylbutyrates ; Receptors, Cell Surface ; free fatty acid 2 receptor, mouse
    Language English
    Publishing date 2021-09-12
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.202100356
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 6280: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top