Amslinger, Sabine (2010) The Tunable Functionality of alpha,beta-Unsaturated Carbonyl Compounds Enables Their Differential Application in Biological Systems. ChemMedChem 5 (3), pp. 351-356.
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alpha,beta-Unsaturated carbonyl compounds as potential drug candidates is a controversial topic since their potential Michael acceptor activity can lead to cell damage and cytotoxicity. Nevertheless, the alpha,beta-unsaturated carbonyl functionality can be employed as a tool to fine tune biological activity by directly manipulating this entity. Depending on their electronic properties, alpha,beta-unsaturated carbonyl functionalities display different reactivities, namely Michael addition, radical scavenging, oxidation or double bond isomerization. Modifying the alpha-position of the alpha,beta-unsaturated carbonyl system, a concept that has not been widely explored, could produce new, very interesting derivatives. Currently in drug development, irreversible binding in active sites has proven to be one answer to drug resistance in cancer treatment. Overall, natural products containing the alpha,beta-unsaturated carbonyl unit possess multiple biological activities that could be transferred into novel pharmaceutical agents.
|Additional information (public):||568KM Times Cited:1 Cited References Count:46|
|Institutions:||Chemistry and Pharmacy > Institut für Organische Chemie > Arbeitskreis Dr. Sabine Amslinger|
|Keywords:||drug design keap1-nrf2 pathway michael addition nf-kappa b alpha,beta-unsaturated carbonyl compounds nitric-oxide production factor-kappa-b tyrosine kinase electrophilic reactivity irreversible inhibitors hepatocyte toxicity antitumor-activity heme oxygenase-1 egf receptor alpha|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Dr. Sabine Amslinger|
|Deposited On:||10 Mar 2011 07:09|
|Last Modified:||10 Mar 2011 10:10|