Literature DB >> 23031595

Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation.

Yanhui Yang1, Andrew Voak, Shane R Wilkinson, Longqin Hu.   

Abstract

A series of potential DFMO prodrugs was designed through the incorporation of 4-nitrobenzyl ester or carbamate groups for potential activation by trypanosomal nitroreductase. It was found that only modification of N(ε)-amino group of DFMO by 4-nitro-2-fluorobenzyloxycarbonyl resulted in significant trypanocidal activity and could serve as a lead for further investigation.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23031595     DOI: 10.1016/j.bmcl.2012.09.005

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation.

Authors:  Michael A Plunk; Alyssa Alaniz; Olatunde P Olademehin; Thomas L Ellington; Kevin L Shuford; Robert R Kane
Journal:  ACS Med Chem Lett       Date:  2020-01-03       Impact factor: 4.345

2.  Design and Catalyzed Activation of Mycophenolic Acid Prodrugs.

Authors:  Michael A Plunk; Jeremy M Quintana; Carly M Darden; Michael C Lawrence; Bashoo Naziruddin; Robert R Kane
Journal:  ACS Med Chem Lett       Date:  2021-04-08       Impact factor: 4.345

Review 3.  Modeling bioavailability to organs protected by biological barriers.

Authors:  Nadia Quignot
Journal:  In Silico Pharmacol       Date:  2013-05-31

4.  Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells.

Authors:  Eva-Maria Herrlinger; Mirjam Hau; Desiree Melanie Redhaber; Gabriele Greve; Dominica Willmann; Simon Steimle; Michael Müller; Michael Lübbert; Christoph Cornelius Miething; Roland Schüle; Manfred Jung
Journal:  Chembiochem       Date:  2020-04-27       Impact factor: 3.164

  4 in total

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