Document Detail


Synthesis and antitumor activities of amino acid prodrugs of amino-combretastatins.
MedLine Citation:
PMID:  10834274     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The synthesis and antitumor activity of water-soluble amino acid prodrugs of amino-combretastatins were reported. Among the synthesized compounds, 7e (CS-39-L-Ser HCI, AC-7700) showed enhanced antitumor activity and decreased toxicity in a Colon 26 murine adenocarcinoma model. Compound 7e showed improved solubility and was easily formulated for in vivo administration. Compound 7e was cleaved to generate the parent compound, CS-39, in the whole blood of mice as well as man, possibly by the action of amino peptidase on the erythrocyte membrane.
Authors:
K Ohsumi; T Hatanaka; R Nakagawa; Y Fukuda; Y Morinaga; Y Suga; Y Nihei; K Ohishi; Y Akiyama; T Tsuji
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Anti-cancer drug design     Volume:  14     ISSN:  0266-9536     ISO Abbreviation:  Anticancer Drug Des.     Publication Date:  1999 Dec 
Date Detail:
Created Date:  2000-06-14     Completed Date:  2000-06-14     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  8603523     Medline TA:  Anticancer Drug Des     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  539-48     Citation Subset:  IM    
Affiliation:
Pharmaceutical Research Laboratories, Ajinomoto Co Inc., Kawasaki, Japan. koji_ohsumi@ajinomoto.com
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MeSH Terms
Descriptor/Qualifier:
Animals
Antineoplastic Agents / chemical synthesis*,  pharmacokinetics,  pharmacology*
Bibenzyls / chemical synthesis*,  pharmacokinetics,  pharmacology
Colonic Neoplasms / drug therapy
Drug Design
Drug Stability
Humans
Hydrogen-Ion Concentration
Hydrolysis
Mice
Mice, Inbred Strains
Neoplasm Transplantation
Prodrugs / chemical synthesis*,  pharmacokinetics,  pharmacology*
Solubility
Tumor Cells, Cultured
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Bibenzyls; 0/Prodrugs

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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