ChemMedChem

Cover image for Vol. 12 Issue 10

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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May 23, 2017

VIP: Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist

VIP: Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor AgonistDr. Daniel Meibom,* Dr. Barbara Albrecht-Küpper,* et al.

Adenosine is the emergency molecule that protects the body from tissue injury during ischemic events. It acts on four different receptors. Activation of adenosine A1 receptors has been shown to be responsible for protective processes in the heart during ischemia, suggesting new options for cardiovascular therapies. However, undesired physiological effects in the heart such as bradycardia and widespread tissue distribution of the A1 receptor makes use of the pharmacological pathways challenging. Read more...

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    Thumbnail image of graphical abstract

    Protoflavones vs. MDR cancer: Two drug efflux pumps, ABCB1 and ABCG2, confer multidrug resistance (MDR) on numerous cancer cell types. New protoflavones were synthesized and tested against a panel of drug-sensitive cancer cells and their MDR counterparts. In vitro studies with various A-ring and 1′-substituted protoflavones revealed derivatives that evade efflux or selectively kill adapted MDR cells. 6-methoxyprotoflavone 1′-O-allyl ether acted with mild MDR selectivity in a murine lymphoma cell line transfected with the human ABCB1 gene.

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