Document Detail


Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
MedLine Citation:
PMID:  22342627     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A set of phenyl-substituted Smac mimetics/IAP inhibitor analogues of lead compound 2a was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compounds 2b-r were prepared and characterized in vitro, using cell-free and cellular assays. Among them, the p-CF(3) substituted analogue 2m showed the best permeability through cell membranes, and was selected for further in vitro and in vivo studies due to its strong, sub-micromolar cellular potency.
Authors:
Aldo Bianchi; Marcello Ugazzi; Luca Ferrante; Daniele Lecis; Cinzia Scavullo; Eloise Mastrangelo; Pierfausto Seneci
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-2-2
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2012 Feb 
Date Detail:
Created Date:  2012-2-20     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Elsevier Ltd. All rights reserved.
Affiliation:
CISI scrl, Via Fantoli 16/15, I-20138 Milan, Italy.
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