Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 5, Pages 1773-1781Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.01.005
Keywords
Peptidomimetics; Biotransformations; Cytostatic/cytotoxic effect; Kinase inhibitors
Funding
- project 'Biotransformations for pharmaceutical and cosmetics industry' [POIG.01.03.01-00-158/09-01]
- European Union within the European Regional Development Fund
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The utility of a novel, chemoenzymatic procedure for the stereocontrolled synthesis of small peptides is presented in the preparation and structure optimisation of dipeptides with cytostatic/cytotoxic activity. The method uses Passerini multicomponent reaction for the preparation of racemic scaffold which is then enantioselectively hydrolysed by hydrolytic enzymes. Products of these transformations are further functionalised towards title compounds. Both activity and selectivity towards tumor cells is optimised. Final compound is shown to be an inhibitor of the protein kinase signaling pathway. (C) 2014 Elsevier Ltd. All rights reserved.
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