Document Detail

Synthesis and antitumor activities of amino acid prodrugs of amino-combretastatins.
MedLine Citation:
PMID:  10834274     Owner:  NLM     Status:  MEDLINE    
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.
K Ohsumi; T Hatanaka; R Nakagawa; Y Fukuda; Y Morinaga; Y Suga; Y Nihei; K Ohishi; Y Akiyama; T Tsuji
Related Documents :
15158954 - New hypoglycaemic agents selected by molecular topology.
7553984 - Screening of tissue cultures and thalli of lichens and some of their active constituent...
12873484 - Pyrimidinone antibiotics--heterocyclic analogues with improved antibacterial spectrum.
20157344 - Synthesis of the naturally occurring (-)-1,3,5-tri-o-caffeoylquinic acid.
22257054 - Advances in the research of β-ketoacyl-acp synthase iii (fabh) inhibitors.
4030514 - Relationship of plasma lipid concentrations to fat deposition in pigs.
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    
Pharmaceutical Research Laboratories, Ajinomoto Co Inc., Kawasaki, Japan.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Antineoplastic Agents / chemical synthesis*,  pharmacokinetics,  pharmacology*
Bibenzyls / chemical synthesis*,  pharmacokinetics,  pharmacology
Colonic Neoplasms / drug therapy
Drug Design
Drug Stability
Hydrogen-Ion Concentration
Mice, Inbred Strains
Neoplasm Transplantation
Prodrugs / chemical synthesis*,  pharmacokinetics,  pharmacology*
Tumor Cells, Cultured
Reg. No./Substance:
0/Antineoplastic Agents; 0/Bibenzyls; 0/Prodrugs

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

Previous Document:  Prodrugs for antibody- and gene-directed enzyme prodrug therapies (ADEPT and GDEPT).
Next Document:  Future directions in health for the new Government: our health and the public health.