Document Detail

Design, synthesis, and evaluation of novel kazusamycin A derivatives as potent antitumor agents.
MedLine Citation:
PMID:  16617017     Owner:  NLM     Status:  MEDLINE    
Novel kazusamycin A derivatives were designed in the viewpoint of decrease of reactivity at the alpha,beta-unsaturated delta-lactone moiety against Michael-type addition. Although 25-30 steps were required for the synthesis of each compound, their syntheses were achieved. Cytotoxicity against HPAC cell line was evaluated, and two of them exhibited comparable potency to kazusamycin A. Hepatic toxicity of these designed compounds was much lower than that of kazusamycin A.
Ryoichi Ando; Yusaku Amano; Hideo Nakamura; Noriyoshi Arai; Isao Kuwajima
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Publication Detail:
Type:  Journal Article     Date:  2006-04-17
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Jun 
Date Detail:
Created Date:  2006-05-08     Completed Date:  2006-08-16     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3315-8     Citation Subset:  IM    
Discovery Technology Laboratory II, Mitsubishi Pharma Corporation, 1000 Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology*,  toxicity
Cell Line, Tumor
Cell Proliferation / drug effects
Drug Design*
Fatty Acids, Unsaturated / chemical synthesis,  chemistry,  pharmacology,  toxicity
Molecular Structure
Structure-Activity Relationship
Reg. No./Substance:
0/Antineoplastic Agents; 0/Fatty Acids, Unsaturated; 94664-05-8/kazusamycin A

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