Document Detail

Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
MedLine Citation:
PMID:  18313309     Owner:  NLM     Status:  MEDLINE    
A series of hybrid compounds of bestatin (1) and actinonin (3), which promote degradation of cellular inhibitor of apoptosis protein 1 (cIAP1), were designed and synthesized. Structure-activity relationship studies indicated that absolute configuration, hydrophobicity at the alpha-position of the internal amide carbonyl group, and the presence of a small substituent at the alpha-position of the ester group are important factors for the expression of potent cIAP1 degradation-promoting activity. HAB-5A (30b) showed the most potent activity (IC(50)=0.53 microM) among the compounds prepared.
Shinichi Sato; Masashi Tetsuhashi; Keiko Sekine; Hiroyuki Miyachi; Mikihiko Naito; Yuichi Hashimoto; Hiroshi Aoyama
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-02-13
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  16     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2008 Apr 
Date Detail:
Created Date:  2008-04-24     Completed Date:  2008-05-21     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  4685-98     Citation Subset:  IM    
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Tokyo 113-0032, Japan.
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MeSH Terms
Apoptosis / drug effects
Cell Line, Tumor
Hydroxamic Acids / chemical synthesis,  chemistry,  pharmacology
Inhibitor of Apoptosis Proteins / genetics*,  metabolism*
Inhibitory Concentration 50
Leucine / analogs & derivatives*,  chemical synthesis,  chemistry,  pharmacology
Molecular Structure
Promoter Regions, Genetic / genetics*
Structure-Activity Relationship
Reg. No./Substance:
0/Hydroxamic Acids; 0/Inhibitor of Apoptosis Proteins; 13434-13-4/actinonin; 58970-76-6/bestatin; 61-90-5/Leucine

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