| Synthesis and antitumour activity of a series of cyclic amidines of 2,3-dihydro-1H-1,5-benzodiazepines. | |
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MedLine Citation:
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PMID: 12109049 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Regina Janciene; Lidija Kosychova; Virginija Bukelskiene; Vigintas Domkus; Zita Stumbreviciūte; Vida Ragaleviciene; Benedikta D Puodziūnaite |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Arzneimittel-Forschung Volume: 52 ISSN: 0004-4172 ISO Abbreviation: Arzneimittelforschung Publication Date: 2002 |
Date Detail:
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Created Date: 2002-07-11 Completed Date: 2002-07-29 Revised Date: 2008-11-21 |
Medline Journal Info:
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Nlm Unique ID: 0372660 Medline TA: Arzneimittelforschung Country: Germany |
Other Details:
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Languages: eng Pagination: 475-81 Citation Subset: IM |
Affiliation:
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Sector of Application of Biologically Active Compounds, Institute of Biochemistry, Vilnius, Lithuania. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents
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chemical synthesis*,
chemistry,
pharmacology* Benzodiazepines / chemical synthesis*, chemistry, pharmacology* Drug Screening Assays, Antitumor Humans Mass Spectrometry Structure-Activity Relationship Tumor Cells, Cultured |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 12794-10-4/Benzodiazepines |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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