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  • Title: Synthesis and antitumour activity of a series of cyclic amidines of 2,3-dihydro-1H-1,5-benzodiazepines.
    Author: Janciene R, Kosychova L, Bukelskiene V, Domkus V, Stumbreviciūte Z, Ragaleviciene V, Puodziūnaite BD.
    Journal: Arzneimittelforschung; 2002; 52(6):475-81. PubMed ID: 12109049.
    Abstract:
    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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