Document Detail

Synthesis and antitumour activity of a series of cyclic amidines of 2,3-dihydro-1H-1,5-benzodiazepines.
MedLine Citation:
PMID:  12109049     Owner:  NLM     Status:  MEDLINE    
2,3-Dihydro-1H-1,5-benzodiazepine amidines were prepared by nucleophilic substitution of 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-2-thiones. Evaluation of the 13 synthesised amidines as antitumour agents was carried out in vitro against 60 human tumour cell lines at the National Cancer Institute, Bethesda, USA. The screening revealed a moderate cell growth inhibition of two derivatives on all cell lines at concentrations ranging from 10(-5) to 10(-4) mol/l. Log P values were theoretically calculated. The more active derivatives were found to exhibit a higher lipophilicity.
Regina Janciene; Lidija Kosychova; Virginija Bukelskiene; Vigintas Domkus; Zita Stumbreviciūte; Vida Ragaleviciene; Benedikta D Puodziūnaite
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  52     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  2002  
Date Detail:
Created Date:  2002-07-11     Completed Date:  2002-07-29     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  475-81     Citation Subset:  IM    
Sector of Application of Biologically Active Compounds, Institute of Biochemistry, Vilnius, Lithuania.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology*
Benzodiazepines / chemical synthesis*,  chemistry,  pharmacology*
Drug Screening Assays, Antitumor
Mass Spectrometry
Structure-Activity Relationship
Tumor Cells, Cultured
Reg. No./Substance:
0/Antineoplastic Agents; 12794-10-4/Benzodiazepines

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