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Steroidal esters of the aromatic nitrogen mustard 2-[4-N,N-bis(2-chloroethyl)amino-phenyl]butanoic acid (2-PHE-BU): synthesis and in-vivo biological evaluation.
MedLine Citation:
PMID:  23187313     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
On the basis of the results of in-silico predictions and in an effort to extend our structure-activity relationship studies, the aromatic nitrogen mustard 2-[4-N,N-bis(2-chloroethyl) amino-phenyl]butanoic acid (2-PHE-BU) was synthesized and conjugated with various steroidal alcohols. The resulting steroidal esters were evaluated for their in-vivo toxicity and antileukemic activity in P388-leukemia-bearing mice. The new derivatives showed significantly reduced toxicity and marginally improved antileukemic activity compared with free 2-PHE-BU. Nevertheless, they did not prove to be superior either to the template steroidal ester used for in-silico predictions or to previously synthesized steroidal esters of aromatic nitrogen mustards. The results obtained indicate that in-silico design predictions may guide the design and synthesis of new bioactive steroidal esters, but further parameters should be considered aiming at the discovery of compounds with optimum activity.
Authors:
Ioanna C Papaconstantinou; Manolis A Fousteris; Anna I Koutsourea; Georgios N Pairas; Athanasios D Papageorgiou; Sotiris S Nikolaropoulos
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Anti-cancer drugs     Volume:  24     ISSN:  1473-5741     ISO Abbreviation:  Anticancer Drugs     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2012-11-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9100823     Medline TA:  Anticancer Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  52-65     Citation Subset:  IM    
Affiliation:
aLaboratory of Medicinal Chemistry, Department of Pharmacy, School of Health Sciences, University of Patras, Patras bLaboratory of Experimental Chemotherapy, Theagenion Anticancer Institute, Thessaloniki, Greece.
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