Document Detail

Synthesis and anticancer activity of geldanamycin derivatives derived from biosynthetically generated metabolites.
MedLine Citation:
PMID:  18175003     Owner:  NLM     Status:  MEDLINE    
A new series of geldanamycin derivatives were synthesized using a semi-synthetic approach involving genetically engineered biosynthetic intermediates. These analogues were then evaluated for anti-proliferation activity in human cancer cell lines, SK-Br3 and SK-Ov3. Most of the synthesized compounds exhibited potent in vitro anti-proliferation activity toward both cell lines. Such compounds potently inhibited the expression of the Hsp90 client protein ErbB2.
Kyeong Lee; Jung S Ryu; Yinglan Jin; Woncheol Kim; Navneet Kaur; Sang J Chung; Yong-Jin Jeon; Joon-Tae Park; Ji S Bang; Hong S Lee; Tae Y Kim; Jung J Lee; Young-Soo Hong
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-11-30
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  6     ISSN:  1477-0520     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2008 Jan 
Date Detail:
Created Date:  2008-01-04     Completed Date:  2008-04-03     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  340-8     Citation Subset:  IM    
Korea Research Institute of Bioscience & Biotechnology, 52 Eoeundong, Yuseonggu, Daejeon, 305-806, Korea.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology*
Benzoquinones / chemical synthesis*,  chemistry,  pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects*
Drug Screening Assays, Antitumor
Genetic Engineering
HSP90 Heat-Shock Proteins / antagonists & inhibitors
Lactams, Macrocyclic / chemical synthesis*,  chemistry,  pharmacology*
Molecular Conformation
Receptor, erbB-2 / antagonists & inhibitors
Reg. No./Substance:
0/Antineoplastic Agents; 0/Benzoquinones; 0/HSP90 Heat-Shock Proteins; 0/Lactams, Macrocyclic; 30562-34-6/geldanamycin; EC protein, human; EC, erbB-2

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