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376 publications
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Functionalization of 9-thioxanthone at the 1-position: From arylaminoderivatives to [1]benzo(thio)pyrano[4,3,2-de]benzothieno[2,3-b]quinolines of biological interest.

Original 1-amino substituted thioxanthone derivatives were easily prepared from the bare heterocycle by a deprotometalation-iodolysis-copper-catalyzed CN bond formation sequence. This last reaction delivered mono- or/and diarylated products depending on the aniline involved.

  • Ref: DOI: 10.1016/j.bioorg.2019.103347
  • Année de publication : 2020
  • Auteurs : MokhtariBrikci-Nigassa N, Nauton L, Moreau P, Mongin O, Duval RE, Picot L, Thiéry V, Souab M, Baratte B, Ruchaud S, Bach S, Le Guevel R, Bentabed-Ababsa G, Erb W, Roisnel T, Dorcet V, Mongin F.
  • Réseaux : Réseaux: « Molécules Marines, Métabolisme et Cancer »
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Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors.

Protein kinases are important drug targets, especially in the area of oncology. This paper reports the synthesis and biological evaluation of new 7-azaindole derivatives bearing benzocycloalkanone motifs as potential protein kinase inhibitors. Four compounds 8g, 8h, 8i, and 8l were discovered to inhibit cyclin-dependent kinase 9 (CDK9/CyclinT) and/or Haspin kinase in the micromolar to nanomolar range.

  • Ref: DOI: 10.1016/j.bmc.2020.115468
  • Année de publication : 2020
  • Auteurs : Qhobosheane MA, Legoabe LJ, Josselin B, Bach S, Ruchaud S, Petzer JP, Beteck RM.
  • Réseaux : Réseaux: « Molécules Marines, Métabolisme et Cancer »
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Autophagy and mitophagy in cancer metabolic remodelling.

Metabolic reprogramming in tumours is now recognized as a hallmark of cancer, participating both in tumour growth and cancer progression. Cancer cells develop global metabolic adaptations allowing them to survive in the low oxygen and nutrient tumour microenvironment.

  • Ref: doi: 10.1016/j.semcdb.2019.05.029
  • Année de publication : 2020
  • Auteurs : Ferro F, Servais S, Besson P, Roger S, Dumas JF, Brisson L.
  • Réseaux : Réseaux: « Molécules Marines, Métabolisme et Cancer »
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Concurrent losses of skeletal muscle mass, adipose tissue and bone mineral density during bevacizumab / cytotoxic…

Changes in skeletal muscle mass (SMM), total adipose tissue mass (TAT) or bone mineral density (BMD) have been described in patients with cancer undergoing various treatments; simultaneous variations of all 3 tissues has not been reported.

  • Ref: doi: 10.1016/j.clnu.2020.02.017
  • Année de publication : 2020
  • Auteurs : Dolly A, Lecomte T, Bouché O, Borg C, Terrebonne E, Douillard JY, Chautard R, Raoul W, Ternant D, Leger J, Bleuzen A, Dumas JF, Servais S, Baracos VE.
  • Réseaux : Réseaux: « Molécules Marines, Métabolisme et Cancer »
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Lipidic synthetic alkaloids as SK3 channel modulators. Synthesis and biological evaluation of 2-substituted tetrahydropyridine derivatives with…

Small Conductance Calcium (Ca2+)-activated potassium (K+) channels (SKCa) are now proved to be involved in many cancer cell behaviors such as proliferation or migration. The SK3 channel isoform was particularly described in breast cancer where it can be associated with the Orai1 Ca2+ channel to form a complex…

  • Ref: doi: 10.1016/j.ejmech.2019.111854
  • Année de publication : 2020
  • Auteurs : Kouba S, Braire J, Félix R, Chantôme A, Jaffrès PA, Lebreton J, Dubreuil D, Pipelier M, Zhang X, Trebak M, Vandier C, Mathé-Allainmat M, Potier-Cartereau M.
  • Réseaux : Réseaux: « Molécules Marines, Métabolisme et Cancer »
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Towards a Stronger Halogen Bond Involving Astatine: Unexpected Adduct with Bu3 PO Stabilized by Hydrogen Bonding.

The halogen bond is a powerful tool for the molecular design and pushing the limits of its strength is of major interest. Bearing the most potent halogen-bond donor atom, astatine monoiodide (AtI) was recently successfully probed [Nat. Chem. 2018, 10, 428-434].

  • Ref: doi: 10.1002/chem.201905389
  • Année de publication : 2020
  • Auteurs : Liu L, Guo N, Champion J, Graton J, Montavon G, Galland N, Maurice R.
  • Réseaux : Réseaux: « Vectorisation, Imagerie, Radiothérapies »
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Secretion of acid sphingomyelinase and ceramide by endothelial cells contributes to radiation-induced intestinal toxicity.

Ceramide-induced endothelial cell apoptosis boosts intestinal stem cell radiosensitivity. However, the molecular connection between these two cellular compartments has not been clearly elucidated.

  • Ref: doi: 10.1158/0008-5472.CAN-19-1527
  • Année de publication : 2020
  • Auteurs : Leonetti D, Estéphan H, Ripoche N, Dubois N, Aguesse A, Gouard S, Brossard L, Chiavassa S, Corre I, Pecqueur C, Neunlist M, Hadchity E, Gaugler MH, Mahé MM, Paris F.
  • Réseaux : Réseaux: « Vectorisation, Imagerie, Radiothérapies »
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Local dose analysis to predict acute and late urinary toxicities after prostate cancer radiotherapy: Assessment of…

To perform bladder dose-surface map (DSM) analysis for (1) identifying symptom-related sub-surfaces (Ssurf) and evaluating their prediction capability of urinary toxicity, (2) comparing DSM with dose-volume map (DVM) (method effect), and (3) assessing the reproducibility of DSM (cohort effect).

  • Ref: doi: 10.1016/j.radonc.2020.02.028
  • Année de publication : 2020
  • Auteurs : Mylona E, Cicchetti A, Rancati T, Palorini F, Fiorino C, Supiot S, Magne N, Crehange G, Valdagni R, Acosta O, de Crevoisier R.
  • Réseaux : Réseaux: « Vectorisation, Imagerie, Radiothérapies »
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Haute Couture or Ready-to-Wear? Tailored Pelvic Radiotherapy for Prostate Cancer Based on Individualized Sentinel Lymph Node…

Prostate cancer (PCa) pelvic radiotherapy fields are defined by guidelines that do not consider individual variations in lymphatic drainage.

  • Ref: doi: 10.3390/cancers12040944
  • Année de publication : 2020
  • Auteurs : Michaud AV, Samain B, Ferrer L, Fleury V, Doré M, Colombié M, Dupuy C, Rio E, Guimas V, Rousseau T, Le Thiec M, Delpon G, Rousseau C, Supiot S.
  • Réseaux : Réseaux: « Vectorisation, Imagerie, Radiothérapies »
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